Site-selective template-directed synthesis of antibody Fc conjugates with concomitant ligand release

Viktoriia Postupalenko, Léo Marx, Mathilde Pantin, David Viertl, Nadège Gsponer, Gaëlle Giudice, Natalia Gasilova, Margret Schottelius, Frédéric Lévy, Patrick Garrouste, Jean-Manuel Segura and Origène Nyanguile

Chem. Sci., 2024, 15, 1324
DOI: 10.1039/D3SC04324J

Chemo- and regio-selective differential modification of native cysteines on an antibody via the use of dehydroalanine forming reagents

Steven Y. Yap, Tobias Butcher, Richard J. Spears, Clíona McMahon, Ioanna A. Thanasi, James R. Baker and Vijay Chudasama

Chem. Sci., 2024, 15, 8557
DOI: 10.1039/D4SC00392F

A CD326 monoclonal antibody modified core cross-linked curcumin-polyphosphoester prodrug for targeted delivery and cancer treatment

Haijiao Li, Mingzu Zhang, Jinlin He, Jian Liu, Xingwei Sun and Peihong Ni

J. Mater. Chem. B, 2023, 11, 9467
DOI: 10.1039/D3TB01703F

The Wittig bioconjugation of maleimide derived, water soluble phosphonium ylides to aldehyde-tagged proteins

Rafael W. Hartmann, Matthijs Pijnappel, Johan Nilvebrant, Hildur Run Helgudottir, Arni Asbjarnarson, Gunnhildur Asta Traustadottir, Thorarinn Gudjonsson, Per-Åke Nygren, Fredrik Lehmann and Luke R. Odell

Org. Biomol. Chem., 2021, 19, 10417
DOI: 10.1039/D1OB01155C

Divinylpyrimidine reagents generate antibody–drug conjugates with excellent in vivo efficacy and tolerability

Stephen J. Walsh, Soleilmane Omarjee, Friederike M. Dannheim, Dominique-Laurent Couturier, Dorentina Bexheti, Lee Mendil, Gemma Cronshaw, Toby Fewster, Charlotte Gregg, Cara Brodie, Jodi L. Miller, Richard Houghton, Jason S. Carroll and David R. Spring

Chem. Commun., 2022, 58, 1962
DOI: 10.1039/D1CC06766D

Bispecific FpFs: a versatile tool for preclinical antibody development

Matthew Collins, Nkiru Ibeanu, Wiktoria Roksana Grabowska, Sahar Awwad, Peng T. Khaw, Steve Brocchini and Hanieh Khalili

RSC Chem. Biol., 2024, 5, 1147
DOI: 10.1039/D4CB00130C

The use of bromopyridazinedione derivatives in chemical biology

Calise Bahou and Vijay Chudasama

Org. Biomol. Chem., 2022, 20, 5879
DOI: 10.1039/D2OB00310D

Bioorthogonal site-selective conjugation of fluorescent dyes to antibodies: method and potential applications

Philipp Grossenbacher, Maria C. Essers, Joël Moser, Simon A. Singer, Stephanie Häusler, Bruno Stieger, Jean-Sébastien Rougier and Martin Lochner

RSC Adv., 2022, 12, 28306
DOI: 10.1039/D2RA05580E

Use of pyridazinediones for tuneable and reversible covalent cysteine modification applied to peptides, proteins and hydrogels

Léa N. C. Rochet, Calise Bahou, Jonathan P. Wojciechowski, Ilias Koutsopetras, Phyllida Britton, Richard J. Spears, Ioanna A. Thanasi, Baihao Shao, Lisha Zhong, Dejan-Krešimir Bučar, Abil E. Aliev, Michael J. Porter, Molly M. Stevens, James R. Baker and Vijay Chudasama

Chem. Sci., 2023, 14, 13743
DOI: 10.1039/D3SC04976K

Visible-light-promoted N–H functionalization of O-substituted hydroxamic acid with diazo esters

Shuangshuang Xia, Yongchan Jian, Liwen Zhang, Cheng Zhang, Yuanyuan An and Yubin Wang

RSC Adv., 2023, 13, 14501
DOI: 10.1039/D3RA02407E

Chemical technology principles for selective bioconjugation of proteins and antibodies

Preeti Chauhan, Ragendu V., Mohan Kumar, Rajib Molla, Surya Dev Mishra, Sneha Basa and Vishal Rai

Chem. Soc. Rev., 2024, 53, 380
DOI: 10.1039/D3CS00715D

Chemical technologies for precise protein bioconjugation interfacing biology and medicine

Mohan Kumar, Neelesh C. Reddy and Vishal Rai

Chem. Commun., 2021, 57, 7083
DOI: 10.1039/D1CC02268G

Multicomponent reactions (MCRs): an emerging toolbox for protein bioconjugation

Joydip Chatterjee, Justin R. Walensky, Sayantan Kundu, Gargi Biswas, Krishnendu Maji and Rajib Sarkar

Org. Biomol. Chem., 2025, 23, 8145
DOI: 10.1039/D5OB01076D

Single and dual functionalization of proteins using site-specific nucleophilic carbon ligations

Qiang Peng, Berlin Zang, Tao Xiong, Chundong Huang, Ting Xu, Chong Zhang, Jun Ren, Fangling Ji and Lingyun Jia

Chem. Commun., 2022, 58, 6316
DOI: 10.1039/D2CC01630C

Site-directed conjugation of single-stranded DNA to affinity proteins: quantifying the importance of conjugation strategy

Andres Rocha Tapia, Fabrice Abgottspon, Johan Nilvebrant, Per-Åke Nygren, Sarah Duclos Ivetich, Andres Javier Bello Hernandez, Ioanna A. Thanasi, Peter A. Szijj, Ghali Sekkat, François M. Cuenot, Vijay Chudasama, Nicola Aceto, Andrew J. deMello and Daniel A. Richards

Chem. Sci., 2024, 15, 8982
DOI: 10.1039/D4SC01838A

Dual reactivity disulfide bridging reagents; enabling new approaches to antibody fragment bioconjugation

Alina Chrzastek, Ioanna A. Thanasi, James A. Irving, Vijay Chudasama and James R. Baker

Chem. Sci., 2022, 13, 11533
DOI: 10.1039/D2SC04531A

NSPs: chromogenic linkers for fast, selective, and irreversible cysteine modification

Yong Hua, Zhi Zou, Alessandro Prescimone, Thomas R. Ward, Marcel Mayor and Valentin Köhler

Chem. Sci., 2024, 15, 10997
DOI: 10.1039/D4SC01710B

Luminescent iridium(iii) 2-cyanobenzothiazole complexes as site-specific labels to afford peptide-based phosphorogenic probes and hydrogels for enzyme activity sensing, cancer imaging and photodynamic therapy

Jun-Wen Xu, Lawrence Cho-Cheung Lee, Alex Man-Hei Yip, Guang-Xi Xu, Peter Kam-Keung Leung and Kenneth Kam-Wing Lo

Inorg. Chem. Front., 2025, 12, 2266
DOI: 10.1039/D4QI03276D

Formation of mono- and dual-labelled antibody fragment conjugates via reversible site-selective disulfide modification and proximity induced lysine reactivity

Ioanna A. Thanasi, Nathalie Bouloc, Clíona McMahon, Ning Wang, Peter A. Szijj, Tobias Butcher, Léa N. C. Rochet, Elizabeth A. Love, Andy Merritt, James R. Baker and Vijay Chudasama

Chem. Sci., 2025, 16, 2763
DOI: 10.1039/D4SC06500J

Degrader-antibody conjugates

Peter S. Dragovich

Chem. Soc. Rev., 2022, 51, 3886
DOI: 10.1039/D2CS00141A

All-in-one disulfide bridging enables the generation of antibody conjugates with modular cargo loading

Friederike M. Dannheim, Stephen J. Walsh, Carolina T. Orozco, Anders Højgaard Hansen, Jonathan D. Bargh, Sophie E. Jackson, Nicholas J. Bond, Jeremy S. Parker, Jason S. Carroll and David R. Spring

Chem. Sci., 2022, 13, 8781
DOI: 10.1039/D2SC02198F

Direct routes to functional RAFT agents from substituted N-alkyl maleimides

Rosa Catania, Ruggero Foralosso, Lampros Spanos, Emanuele Russo, Francesca Mastrotto, Pratik Gurnani, Kevin Butler, Huw Williams, Snow Stolnik and Giuseppe Mantovani

Polym. Chem., 2022, 13, 6261
DOI: 10.1039/D1PY01565F

Antibody dual-functionalisation enabled through a modular divinylpyrimidine disulfide rebridging strategy

Abigail R. Hanby, Stephen J. Walsh, Andrew J. Counsell, Nicola Ashman, Kim T. Mortensen, Jason S. Carroll and David R. Spring

Chem. Commun., 2022, 58, 9401
DOI: 10.1039/D2CC02515A

Technical, preclinical, and clinical developments of Fc-glycan-specific antibody–drug conjugates

Qiang Yang and Yunpeng Liu

RSC Med. Chem., 2025, 16, 50
DOI: 10.1039/D4MD00637B

A platform for SpyCatcher conjugation to native antibodies

Sona Krajcovicova, Thomas Wharton, Claudia L. Driscoll, Thomas A. King, Mark R. Howarth and David R. Spring

Chem. Sci., 2025, 16, 10602
DOI: 10.1039/D5SC02286J

Enabling the formation of native mAb, Fab′ and Fc-conjugates using a bis-disulfide bridging reagent to achieve tunable payload-to-antibody ratios (PARs)

Fabien Thoreau, Léa N. C. Rochet, James R. Baker and Vijay Chudasama

Chem. Sci., 2023, 14, 3752
DOI: 10.1039/D2SC06318B

Prodrugs as empowering tools in drug discovery and development: recent strategic applications of drug delivery solutions to mitigate challenges associated with lead compounds and drug candidates

Murugaiah A. M. Subbaiah, Jarkko Rautio and Nicholas A. Meanwell

Chem. Soc. Rev., 2024, 53, 2099
DOI: 10.1039/D2CS00957A

A dual-enzyme cleavable linker for antibody–drug conjugates

Jonathan D. Bargh, Stephen J. Walsh, Nicola Ashman, Albert Isidro-Llobet, Jason S. Carroll and David R. Spring

Chem. Commun., 2021, 57, 3457
DOI: 10.1039/D1CC00957E

Rapid and robust cysteine bioconjugation with vinylheteroarenes

Hikaru Seki, Stephen J. Walsh, Jonathan D. Bargh, Jeremy S. Parker, Jason Carroll and David R. Spring

Chem. Sci., 2021, 12, 9060
DOI: 10.1039/D1SC02722K

Generation of antibody–drug conjugates by proximity-driven acyl transfer and sortase-mediated ligation

Zhi-Hui Cui, Hua Zhang, Feng-Hao Zheng, Jun-Hao Xue, Qing-Hong Yin, Xiao-Lei Xie, Yu-Xuan Wang, Tao Wang, Li Zhou and Ge-Min Fang

Org. Biomol. Chem., 2025, 23, 188
DOI: 10.1039/D4OB01624F

Transglutaminase-mediated proximity labeling of a specific Lys residue in a native IgG antibody

Riko Nishioka, Ryuya Iida, Kosuke Minamihata, Ryo Sato, Michio Kimura and Noriho Kamiya

Chem. Commun., 2024, 60, 8545
DOI: 10.1039/D4CC01728E

Compact hydrophilic electrophiles enable highly efficacious high DAR ADCs with excellent in vivo PK profile

Philipp Ochtrop, Jahaziel Jahzerah, Paul Machui, Isabelle Mai, Dominik Schumacher, Jonas Helma, Marc-André Kasper and Christian P. R. Hackenberger

Chem. Sci., 2023, 14, 2259
DOI: 10.1039/D2SC05678J

Tyrosine bioconjugation with hypervalent iodine

Nina Declas, John R. J. Maynard, Laure Menin, Natalia Gasilova, Sebastian Götze, Jakob L. Sprague, Pierre Stallforth, Stefan Matile and Jerome Waser

Chem. Sci., 2022, 13, 12808
DOI: 10.1039/D2SC04558C

Enabling the next steps in cancer immunotherapy: from antibody-based bispecifics to multispecifics, with an evolving role for bioconjugation chemistry

Fabien Thoreau and Vijay Chudasama

RSC Chem. Biol., 2022, 3, 140
DOI: 10.1039/D1CB00082A

Disulfide re-bridging reagents for single-payload antibody-drug conjugates

Thomas A. King, Stephen J. Walsh, Mia Kapun, Thomas Wharton, Sona Krajcovicova, Melanie S. Glossop and David R. Spring

Chem. Commun., 2023, 59, 9868
DOI: 10.1039/D3CC02980H

Enabling the synthesis of multi-payload thio-antibody conjugates through the use of pyridazinediones, p-anisidine derivatives and various click chemistries

Clíona McMahon, Christophe J. Queval, Ioanna A. Thanasi, Dawn H. W. Lau, Michael Howell, Ning Wang, Maximillian T. W. Lee, Josephine S. Gaynord, James R. Baker and Vijay Chudasama

RSC Chem. Biol., 2026
DOI: 10.1039/D6CB00018E

Two birds one stone: β-fluoropyrrolyl-cysteine SNAr chemistry enabling functional porphyrin bioconjugation

Guo-Qing Jin, Jing-Xiang Wang, Jianhua Lu, Hang Zhang, Yuhang Yao, Yingying Ning, Hua Lu, Song Gao and Jun-Long Zhang

Chem. Sci., 2023, 14, 2070
DOI: 10.1039/D2SC06209G

Modification of bacterial microcompartments with target biomolecules via post-translational SpyTagging

David M Beal, Mingzhi Liang, Ian Brown, James D Budge, Emily R Burrows, Kevin Howland, Phoebe Lee, Sarah Martin, Andrew Morrell, Emi Nemoto-Smith, Joanne Roobol, Maria Stanley, C Mark Smales and Martin J Warren

Mater. Adv., 2023, 4, 2963
DOI: 10.1039/D3MA00071K

Template directed synthesis of antibody Fc conjugates with concomitant ligand release

Viktoriia Postupalenko, Léo Marx, David Viertl, Nadège Gsponer, Natalia Gasilova, Thibaut Denoel, Niklaus Schaefer, John O. Prior, Gerrit Hagens, Frédéric Lévy, Patrick Garrouste, Jean-Manuel Segura and Origène Nyanguile

Chem. Sci., 2022, 13, 3965
DOI: 10.1039/D1SC06182H

Catalyst-free electrosynthesis of benzothiophenes from 2-alkenylaryl disulfides

Juyeong Lee, Eunsoo Yu and Cheol-Min Park

Org. Biomol. Chem., 2022, 20, 7499
DOI: 10.1039/D2OB01402E

Unearthing the unique stability of thiophosphonium-C-terminal cysteine adducts on peptides and proteins

Richard J. Spears, Alina Chrzastek, Steven Y. Yap, Kersti Karu, Abil E. Aliev, James R. Baker and Vijay Chudasama

Chem. Commun., 2022, 58, 5359
DOI: 10.1039/D2CC01090A

Recent developments in chemical conjugation strategies targeting native amino acids in proteins and their applications in antibody–drug conjugates

Min Sun Kang, Theresa Wai See Kong, Joycelyn Yi Xin Khoo and Teck-Peng Loh

Chem. Sci., 2021, 12, 13613
DOI: 10.1039/D1SC02973H

Selenium chemistry for spatio-selective peptide and protein functionalization

Zhenguang Zhao, Shay Laps, Jacob S. Gichtin and Norman Metanis

Nat Rev Chem, 2024, 8, 211
DOI: 10.1038/s41570-024-00579-1

Uncovering potential targets for antibody-drug conjugates in the treatment of gynecologic malignancies

Yuying Jiang, Yuance Xu, Junqi He, Lei Sui, Tian Li, Nannan Xia and Qin Yao

Front. Pharmacol., 2025, 16
DOI: 10.3389/fphar.2025.1525733

A Traceless Site‐Specific Conjugation on Native Antibodies Enables Efficient One‐Step Payload Assembly

Yue Zeng, Wei Shi, Qian Dong, Wanzhen Li, Jianxin Zhang, Xuelian Ren, Caihong Tang, Bo Liu, Yuanli Song, Yali Wu, Xingxing Diao, Hu Zhou, He Huang, Feng Tang and Wei Huang

Angew Chem Int Ed, 2022, 61
DOI: 10.1002/anie.202204132

Beyond R-CHOP: The rise of antibody-drug conjugates in DLBCL

Xiaoxiao Xu, Meichen Liu and Zhenxing Wang

Blood Reviews, 2026, 101363
DOI: 10.1016/j.blre.2026.101363

An Efficient Opal‐Suppressor Tryptophanyl Pair Creates New Routes for Simultaneously Incorporating up to Three Distinct Noncanonical Amino Acids into Proteins in Mammalian Cells**

Arianna O. Osgood, Yunan Zheng, Soumya Jyoti Singha Roy, Nikolaos Biris, Myer Hussain, Conor Loynd, Delilah Jewel, James S. Italia and Abhishek Chatterjee

Angew Chem Int Ed, 2023, 62
DOI: 10.1002/anie.202219269

New analytical challenges in characterization of antibody-drug conjugates

Erika Maria Ricci, Enrico Dainese, Vincenzo De Laurenzi, Giulio Lovato, Gianluca Sala, Marcello Locatelli and Miryam Perrucci

Journal of Chromatography Open, 2025, 8, 100260
DOI: 10.1016/j.jcoa.2025.100260

Developing analytical ion exchange chromatography methods for antibody drug conjugates containing the hydrolysis-prone succinimide-thioether conjugation chemistry

Jessica Webb, Chendi Niu, Benjamin Ritter, Methal Albarghouthi, Xiaoyu Chen and Chunlei Wang

Journal of Pharmaceutical Sciences, 2024, 113, 3279
DOI: 10.1016/j.xphs.2024.08.021

Multivalent linkers: A growing trend in antibody–drug conjugate development

Evgeny L. Gulyak, Vladimir A. Korshun and Ksenia A. Sapozhnikova

Biotechnology Advances, 2026, 89, 108841
DOI: 10.1016/j.biotechadv.2026.108841

Investigating a Boronate‐Affinity‐Guided Acylation Reaction for Labelling Native Antibodies

Avijit K. Adak, Kuan‐Ting Huang, Chien‐Yu Liao, Yuan‐Jung Lee, Wen‐Hua Kuo, Yi‐Ren Huo, Pei‐Jhen Li, Yi‐Ju Chen, Bo‐Shiun Chen, Yu‐Ju Chen, Kuo Chu Hwang, Wun‐Shang Wayne Chang and Chun‐Cheng Lin

Chemistry A European J, 2022, 28
DOI: 10.1002/chem.202104178

Strategies for UF/DF-Based Impurity Removal in the Post-conjugation Purification of Antibody–Drug Conjugates

Lara Fernandez-Cerezo, Melissa Holstein, Srinath Thirumalairajan, Dante Romanini, Pavlo Kos, Thomas Raglione and Paul G. Bulger

Org. Process Res. Dev., 2023, 27, 1258
DOI: 10.1021/acs.oprd.3c00137

Site‐Specific Modification of Native IgGs with Flexible Drug‐Load

Jöri E. Wehrmüller, Julia C. Frei, Torsten Hechler, Michael Kulke, Andreas Pahl, Martin Béhé, Roger Schibli and Philipp R. Spycher

ChemBioChem, 2025, 26
DOI: 10.1002/cbic.202400511

Modification of Cysteine-Substituted Antibodies Using Enzymatic Oxidative Coupling Reactions

Wendy Cao, Johnathan C. Maza, Natalia Chernyak, John A. Flygare, Shane W. Krska, F. Dean Toste and Matthew B. Francis

Bioconjugate Chem., 2023, 34, 510
DOI: 10.1021/acs.bioconjchem.2c00576

Traceless Peptide and Protein Modification via Rational Tuning of Pyridiniums

Chuan Wan, Yichi Zhang, Jinpeng Wang, Yun Xing, Dongyan Yang, Qinhong Luo, Jianbo Liu, Yuxin Ye, Zhihong Liu, Feng Yin, Rui Wang and Zigang Li

J. Am. Chem. Soc., 2024, 146, 2624
DOI: 10.1021/jacs.3c11864

Functionalized protein nanopores: Strategies and applications

Ke Sun, Mengze Wu, Yu Xin, Yue Li, Minghan Li, Jinna Wang, Yuan Ju, Shengli Zhang and Jia Geng

Nano Research, 2026, 19, 94908343
DOI: 10.26599/NR.2026.94908343

Recent developments in bioconjugation: From strategies to design and clinical applications

Faezeh Samieipour, Hassan Dianat-Moghadam and Hossein Khanahmad

Biomedicine & Pharmacotherapy, 2025, 192, 118593
DOI: 10.1016/j.biopha.2025.118593

Design of high avidity and low affinity antibodies for in situ control of antibody drug conjugate targeting

Reginald Evans and Greg M. Thurber

Sci Rep, 2022, 12
DOI: 10.1038/s41598-022-11648-0

Manipulating gene expression levels in mammalian cell factories: An outline of synthetic molecular toolboxes to achieve multiplexed control

Peter Eisenhut, Nicolas Marx, Giulia Borsi, Maja Papež, Caterina Ruggeri, Martina Baumann and Nicole Borth

New Biotechnology, 2024, 79, 1
DOI: 10.1016/j.nbt.2023.11.003

Approaches towards tissue‐selective pharmacology of the mineralocorticoid receptor

Dorien Clarisse, Lisa Deng, Karolien de Bosscher and Achim Lother

British J Pharmacology, 2022, 179, 3235
DOI: 10.1111/bph.15719

Self‐Assembled L–DNA Linkers for Rapid Construction of Multi‐Specific Antibody‐Drug Conjugates Library

Liujuan Zhou, Fan Yang, Zhaoshuai Bai, Xiaohui Zhou, Zhihai Zhang, Zhihang Li, Junyuan Gong, Junqi Yu, Liqiang Pan, Chan Cao and James J. Chou

Angew Chem Int Ed, 2023, 62
DOI: 10.1002/anie.202302805

Reactivity and Selectivity Principles in Native Protein Bioconjugation

Ramesh Adakkattil, Kalyani Thakur and Vishal Rai

The Chemical Record, 2021, 21, 1941
DOI: 10.1002/tcr.202100108

Polymersome Membrane Engineering with Active Targeting or Controlled Permeability for Responsive Drug Delivery

Anum Kayani, Arsalan Raza, Jiale Si, Debabrata Dutta, Qinghao Zhou and Zhishen Ge

Biomacromolecules, 2023, 24, 4622
DOI: 10.1021/acs.biomac.3c00839

Chemical Conjugation to Less Targeted Proteinogenic Amino Acids

Nanna L. Kjærsgaard, Thorbjørn B. Nielsen and Kurt V. Gothelf

ChemBioChem, 2022, 23
DOI: 10.1002/cbic.202200245

Peptide Tags for Site‐Selective Nonenzymatic Covalent Modification of Proteins

Delphine Nørgaard Møller, Christian Kofoed, Mikkel Boas Thygesen and Knud J. Jensen

Journal of Peptide Science, 2025, 31
DOI: 10.1002/psc.70058

Generation of DAR1 Antibody-Drug Conjugates for Ultrapotent Payloads Using Tailored GlycoConnect Technology

Laureen de Bever, Sorraya Popal, Jord van Schaik, Baron Rubahamya, Floris L. van Delft, Greg M. Thurber and Sander S. van Berkel

Bioconjugate Chem., 2023, 34, 538
DOI: 10.1021/acs.bioconjchem.2c00611

Multiplexed Quantitative Analysis of Antibody–Drug Conjugates with Labile CBI-Dimer Payloads In Vivo Using Immunoaffinity LC-MS/MS

Suk-Joon Hyung, Douglas D. Leipold, Donna W. Lee, Surinder Kaur and Ola M. Saad

Anal. Chem., 2022, 94, 1158
DOI: 10.1021/acs.analchem.1c04338

NBS-Promoted Synthesis of Maleimides by Oxidative Dearomatization of Pyrroles: Mechanistic Investigations Using Online MS in Real-Time

Ankit Kumar, Pawan K. Mishra, Abhijit Nandy, Ryan A. Altman, Shibdas Banerjee and Akhilesh K. Verma

Org. Lett., 2025, 27, 7810
DOI: 10.1021/acs.orglett.5c01976

Electric-Field-Mediated In-Sensor Alignment of Antibody’s Orientation to Enhance the Antibody–Antigen Binding for Ultrahigh Sensitivity Sensors

Hye Jin Kim, Dongsung Park, Yejin Park, Dae-Hyeong Kim and Jinsik Kim

Nano Lett., 2022, 22, 6537
DOI: 10.1021/acs.nanolett.2c01584

Site-Specific Synthesis of Protein-Oligo Conjugates through Histidine-Maleimide-Mediated Imidazolidinone Formation

Chun Guo, Kang Xu, Chen Chen, Jianpeng Wang and Hong Li

Bioconjugate Chem., 2022, 33, 1885
DOI: 10.1021/acs.bioconjchem.2c00350

Site-oriented conjugation of poly(2-methacryloyloxyethyl phosphorylcholine) for enhanced brain delivery of antibody

Jie Ren, Chloe E. Jepson, Sarah L. Nealy, Charles J. Kuhlmann, Satoru Osuka, Stella Uloma Azolibe, Madison T. Blucas, Yoshiko Nagaoka-Kamata, Eugenia Kharlampieva and Masakazu Kamata

Front. Cell Dev. Biol., 2023, 11
DOI: 10.3389/fcell.2023.1214118

CD4 Mimic‐Neutralizing Antibody Conjugates Synthesized by Site‐Specific Modification Methods as HIV‐1 Entry Inhibitors

Kohei Tsuji, Yutaro Miura, Takeo Kuwata, Riku Matsuzaki, Takuya Kobayakawa, Kaho Matsumoto, Yuji Ito, Taku Yoshiya, Shuzo Matsushita and Hirokazu Tamamura

ChemMedChem, 2026, 21
DOI: 10.1002/cmdc.202500820

Utilizing Constrained Bicyclic Peptides for In Vitro Diagnostics

André Shamsabadi, Adam Creamer, Christy J. Sadler, Aida Abdelwahed, Katherine U. Gaynor, Yuliya Demydchuk, Gabriela Ivanova-Berndt, Katerine Van Rietschoten, Paul Beswick, Liuhong Chen, Gustavo Arruda Bezerra, Aleksei Lulla, Paul Brear, Marko Hyvönen, Michael J. Skynner and Molly M. Stevens

ACS Nano, 2026, 20, 5928
DOI: 10.1021/acsnano.5c19041

Multi-attribute methods in antibody-drug conjugate characterization and quality control: Opportunities, challenges, and regulatory outlook

Devendra Kumar and Neerja Trivedi

Journal of Chromatography A, 2026, 1768, 466711
DOI: 10.1016/j.chroma.2026.466711

The first ADC bearing the ferroptosis inducer RSL3 as a payload with conservation of the fragile electrophilic warhead

Kim-Anh Nguyen, Louise Conilh, Pierre Falson, Charles Dumontet and Ahcène Boumendjel

European Journal of Medicinal Chemistry, 2022, 244, 114863
DOI: 10.1016/j.ejmech.2022.114863

A review of conjugation technologies for antibody drug conjugates

Qirui Fan, Hu Chen, Guoguang Wei, Ding Wei, Zekun Wang, Lin Zhang, Jun Wang and Marie Zhu

Antibody Therapeutics, 2025, 8, 157
DOI: 10.1093/abt/tbaf010

Integrated strategy for biotransformation of antibody–drug conjugates and multidimensional interpretation via high-resolution mass spectrometry

Ziyi Li, Jingxian Zhang, Yue Wu, Fan Wang and Tingting Cai

Drug Metabolism and Disposition, 2025, 53, 100081
DOI: 10.1016/j.dmd.2025.100081

Toward Homogenous Antibody Drug Conjugates Using Enzyme-Based Conjugation Approaches

Ahmad Hussain, Armin Grimm, Wenjie Sheng, Chaoyu Zhang, Marwah Al-Rawe, Karen Bräutigam, Mobarak Abu Mraheil, Felix Zeppernick and Ivo Meinhold-Heerlein

Pharmaceuticals, 2021, 14, 343
DOI: 10.3390/ph14040343

Bioconjugation Techniques for Enhancing Stability and Targeting Efficiency of Protein and Peptide Therapeutics

Tanuja Bisht, Anupriya Adhikari, Shivanand Patil and Shivang Dhoundiyal

CPPS, 2024, 25, 226
DOI: 10.2174/0113892037268777231013154850

Bispecific antibodies for targeted delivery of anti-cancer therapeutic agents: A review

Adilet Beishenaliev, Yean Leng Loke, Sook Jing Goh, Hui Nee Geo, Malar Mugila, Misni Misran, Lip Yong Chung, Lik Voon Kiew, Steve Roffler and Yin Yin Teo

Journal of Controlled Release, 2023, 359, 268
DOI: 10.1016/j.jconrel.2023.05.032

Monoclonal antibodies in breast cancer: A critical appraisal

Akanksha Behl, Zahoor A. Wani, Nagendra Nath Das, Virinder S. Parmar, Christophe Len, Shashwat Malhotra and Anil K. Chhillar

Critical Reviews in Oncology/Hematology, 2023, 183, 103915
DOI: 10.1016/j.critrevonc.2023.103915

Scale-Up Synthesis of Site-Specific Antibody–Drug Conjugates Using AJICAP Second-Generation Technology

Tomohiro Watanabe, Tomohiro Fujii, Jason T. Stofleth, Rika Takasugi, Kazutoshi Takahashi and Yutaka Matsuda

Org. Process Res. Dev., 2023, 27, 1136
DOI: 10.1021/acs.oprd.3c00111

Prospects for the Use of Antibody-Drug Conjugates in Cancer Therapy

A. O. Makarova, E. V. Svirshchevskaya, M. M. Titov, S. M. Deyev and R. V. Kholodenko

Russ J Bioorg Chem, 2025, 51, 556
DOI: 10.1134/S1068162024605597

Ligand-Directed Site-Selective Cysteine Bioconjugation of the KELCH Domain of KEAP1 with Hypervalent Iodine Reagents

Christine Marty, Xinjian Ji, Stefano Nicolai, Christian Heinis and Jerome Waser

J. Am. Chem. Soc., 2025, 147, 42524
DOI: 10.1021/jacs.5c13391

Site-Specific Glycan Conjugation Improves Stability and Efficacy of an Antibody–Drug Conjugates Bearing DXd as a Cytotoxic Payload

Shino Manabe, Shogo Senga, Shogo Iwamoto, Hikaru Yarita, Ryo Takahashi, Ai Mitani, Wataru Sumiyoshi, Asako Hoshinoo, Methanee Hiranyakorn, Takashi Kinoshita and Chihoko Yoshimura

ACS Omega, 2026, 11, 13459
DOI: 10.1021/acsomega.5c10898

Recent advances in N- and C-terminus cysteine protein bioconjugation

Richard J. Spears and Vijay Chudasama

Current Opinion in Chemical Biology, 2023, 75, 102306
DOI: 10.1016/j.cbpa.2023.102306

Creating an Unusual Glycine-Rich Motif in a Peptide Amidase Leads to Versatile Protein C-Terminal Traceless Functionalization

Tong Zhu, Yinglu Cui, Wenchao Geng, Guoxia Liu, Huifeng Jiang, Ruifeng Li and Bian Wu

ACS Catal., 2022, 12, 8019
DOI: 10.1021/acscatal.2c01456

Precision Medicine in Rheumatic Diseases: Unlocking the Potential of Antibody-Drug Conjugates

Zhiwen Huang, Zachary Braunstein, Jun Chen, Yingying Wei, Xiaoquan Rao, Lingli Dong and Jixin Zhong

Pharmacological Reviews, 2024, 76, 579
DOI: 10.1124/pharmrev.123.001084

One‐Step Maleimide‐Based Dual Functionalization of Protein N‐Termini

Kengo Hanaya, Kazuaki Taguchi, Yuki Wada and Masaki Kawano

Angew Chem Int Ed, 2025, 64
DOI: 10.1002/anie.202417134

Bisulfite Radical (HSO3•)-Mediated Modular Strategy for Synthesis of Aliphatic Sulfonate Esters

Yongxin Zhang, Hui Xu, Ligang Huang, Zhiming Zhu, Ziyang Li, Jiang Duan and Chao Shu

ACS Catal., 2025, 15, 13145
DOI: 10.1021/acscatal.5c02630

Stoichiometric Antibody–Polymer–Drug Conjugate for Effective Low-Dose Treatment of Breast Cancer

Victor Lehot, Ondřej Lidický, Julien Most, Marc Nothisen, Stéphane Erb, Igor Dovgan, Artem Osypenko, Oleksandr Koniev, Sergii Kolodych, Lenka Kotrchová, Guilhem Chaubet, Sarah Cianférani, Tomáš Etrych and Alain Wagner

Biomacromolecules, 2025, 26, 7309
DOI: 10.1021/acs.biomac.5c00598

A Genetically Encoded Photocaged Cysteine for Facile Site-Specific Introduction of Conjugation-Ready Thiol Residues in Antibodies

Arianna O. Osgood, Soumya Jyoti Singha Roy, David Koo, Renpeng Gu and Abhishek Chatterjee

Bioconjugate Chem., 2024, 35, 457
DOI: 10.1021/acs.bioconjchem.3c00513

Recent Advances in Targeted Cancer Therapy: Are PDCs the Next Generation of ADCs?

Baochen Zhang, Mo Wang, Li Sun, Jiawei Liu, Libinghan Yin, Mingjing Xia, Ling Zhang, Xifu Liu and Yu Cheng

J. Med. Chem., 2024, 67, 11469
DOI: 10.1021/acs.jmedchem.4c00106

Bioproduction Platform to Generate Functionalized Disulfide-Constrained Peptide Analogues

Sunhee Hwang, Aaron T. Balana, Bryan Martin, Michael Clarkson, Paola Di Lello, Hao Wu, Yanjie Li, Jakob Fuhrmann, Yavuz Dagdas, Patrick Holder, Christina I. Schroeder, Stephen E. Miller and Xinxin Gao

ACS Bio Med Chem Au, 2024, 4, 190
DOI: 10.1021/acsbiomedchemau.4c00026

Preclinical Antitumor Efficacy of a Novel Anti–c-Kit Antibody–Drug Conjugate, NN3201, in c-Kit–Positive Tumors

Chansik Kim, Jinwoo Park, Jin-Ock Kim, Han-Jik Ko, Jin Gu Cho, Yeonjy Lee, Jina Lee, TaeMin Wi, Jiwoo Moon, Sohyeon Park, Jaeyoung Song, Sun-Hwa Lee, Gong Sung and Sang Gyu Park

Molecular Cancer Therapeutics, 2026, 25, 34
DOI: 10.1158/1535-7163.MCT-25-0396

Bispecific antibody drug conjugates: Making 1+1>2

Yilin Gu, Zhijia Wang and Yuxi Wang

Acta Pharmaceutica Sinica B, 2024, 14, 1965
DOI: 10.1016/j.apsb.2024.01.009

Aminooxy Click Modification of a Periodate-Oxidized Immunoglobulin G: A General Approach to Antibody–Drug Conjugates with Dye-Mediated Expeditious Stoichiometry Control

Ksenia A. Sapozhnikova, Evgeny L. Gulyak, Vladimir A. Brylev, Vsevolod A. Misyurin, Sergey D. Oreshkov, Anastasiya V. Alexeeva, Dmitry Yu. Ryazantsev, Maria A. Simonova, Ekaterina V. Ryabukhina, Galina P. Popova, Nataliya A. Tikhonova, Natalia A. Lyzhko, Alexander E. Barmashov, Andrey V. Misyurin, Alexey V. Ustinov, Vera A. Alferova and Vladimir A. Korshun

IJMS, 2023, 24, 5134
DOI: 10.3390/ijms24065134

Phenyldivinylsulfonamides for the construction of antibody–drug conjugates with controlled four payloads

Ding Wei, Yuecheng Jiang, Yurong Mao, Zili Xu, Jiakang Chen, Xiuxia Gao, Jiusheng Li, Biao Jiang and Hongli Chen

Bioorganic Chemistry, 2023, 134, 106463
DOI: 10.1016/j.bioorg.2023.106463

DNA–drug conjugates enable logic-gated drug delivery amplified by hybridization chain reactions

Si-Kai Chen, Miguel López-Tena, Francesco Russo, Emma E. Watson, Millicent Dockerill, Javier Cabello Garcia, Sofia Barluenga and Nicolas Winssinger

Nat Biotechnol, 2026
DOI: 10.1038/s41587-026-03044-0

Antibody drug conjugates in breast cancer in China: Highlights, challenges, and prospects

Jianbin Li and Zefei Jiang

Cancer, 2024, 130, 1371
DOI: 10.1002/cncr.35093

Cetuximab–Polymersome–Mertansine Nanodrug for Potent and Targeted Therapy of EGFR-Positive Cancers

Shujing Yue, Yifan Zhang, Yaohua Wei, Rainer Haag, Huanli Sun and Zhiyuan Zhong

Biomacromolecules, 2022, 23, 100
DOI: 10.1021/acs.biomac.1c01065

RGD and Scutellarin Conjugate (WK001) Targeting Platelet Glycoprotein IIb/IIIa Receptor Protects from Myocardial Ischemia/Reperfusion Injury: Synthesis, Characterization, and Bioactivity Evaluation

Lancong Liu, Wenfeng Ding, Lili He, Yi Yang, Fuyi Guan, Xinlin Sun, Yan Peng, Xue Chen, Wenhao Zhao, Yu Xiao and Pei Luo

Bioconjugate Chem., 2023, 34, 477
DOI: 10.1021/acs.bioconjchem.2c00439

A Review on the Stability Challenges of Advanced Biologic Therapeutics

Sruthi Sarvepalli, Shashank Reddy Pasika, Vartika Verma, Anusha Thumma, Sandeep Bolla, Pavan Kumar Nukala, Arun Butreddy and Pradeep Kumar Bolla

Pharmaceutics, 2025, 17, 550
DOI: 10.3390/pharmaceutics17050550

Immune checkpoint-targeted drug conjugates: A promising tool for remodeling tumor immune microenvironment

Jiwoong Choi, Hochung Jang, Jiwon Choi, Yeonho Choi, Yoosoo Yang, Man Kyu Shim and Sun Hwa Kim

Journal of Controlled Release, 2023, 359, 85
DOI: 10.1016/j.jconrel.2023.05.031

Enzymatic glycan remodeling–metal free click (GlycoConnect™) provides homogenous antibody-drug conjugates with improved stability and therapeutic index without sequence engineering

Marloes A. Wijdeven, Remon van Geel, Jorin H. Hoogenboom, Jorge M. M. Verkade, Brian M. G. Janssen, Inge Hurkmans, Laureen de Bever, Sander S. van Berkel and Floris L. van Delft

mAbs, 2022, 14
DOI: 10.1080/19420862.2022.2078466

Homogeneous antibody-drug conjugates with dual payloads: potential, methods and considerations

Miao Wen, Abigail Yu, Young Park, Daniel Calarese, Hans-Peter Gerber and Gang Yin

mAbs, 2025, 17
DOI: 10.1080/19420862.2025.2498162

What influences the activity of Degrader−Antibody conjugates (DACs)

Yaolin Guo, Xiaoxue Li, Yang Xie and Yuxi Wang

European Journal of Medicinal Chemistry, 2024, 268, 116216
DOI: 10.1016/j.ejmech.2024.116216

Mechanisms of ADC Toxicity and Strategies to Increase ADC Tolerability

Toan D. Nguyen, Brandon M. Bordeau and Joseph P. Balthasar

Cancers, 2023, 15, 713
DOI: 10.3390/cancers15030713

From Life in the Sea to the Clinic: The Marine Drugs Approved and under Clinical Trial

Emiliano Cappello and Paola Nieri

Life, 2021, 11, 1390
DOI: 10.3390/life11121390

Proximity-based site-specific labeling of a native IgG Fab fragment by a fusion microbial transglutaminase-protein G variant

Koki Murozono, Riko Nishioka, Yoshirou Kawaguchi, Michio Kimura and Noriho Kamiya

New Biotechnology, 2025, 90, 56
DOI: 10.1016/j.nbt.2025.08.004

Photochemical oxidative coupling of thiols to disulfides using Bi quantum dots: Mild and efficient catalysis

Haiyan Xu, Yuanyuan Huang, Yinchun Liang, Nan Wang, Dejun Dong, Mengke Wang, Weichun Huang, You Zi and Zhanping Yang

Synthetic Communications, 2024, 54, 1482
DOI: 10.1080/00397911.2024.2392187

Degrader–Antibody Conjugates: Emerging New Modality

Ki Bum Hong and Hongchan An

J. Med. Chem., 2023, 66, 140
DOI: 10.1021/acs.jmedchem.2c01791

Second Generation Tiancimycin-Based Antibody–Drug Conjugates Enabled by Highly Efficient Semi-synthetic Approach Specifically Targeting B-Cell Malignancies

Alexander F. Kiefer, Pankajavalli Thirugnanasambantham, Yuan Jin, Andrew D. Steele, Dobeen Hwang, Yanlong Jiang, Ajeeth Adhikari, Dong Yang, Jing Chang, Rakeb Tafesse, Christoph Rader, Natarajan Muthusamy and Ben Shen

JACS Au, 2025, 5, 3171
DOI: 10.1021/jacsau.5c00353

OaAEP1 Ligase-Assisted Chemoenzymatic Synthesis of Full Cysteine-Rich Metal-Binding Cyanobacterial Metallothionein SmtA

Anastasiia Antonenko, Avinash Kumar Singh, Karolina Mosna and Artur Krężel

Bioconjugate Chem., 2023, 34, 719
DOI: 10.1021/acs.bioconjchem.3c00037

Renal Clearable Quantum Dot–Drug Conjugates Modulate Labile Iron Species and Scavenge Free Radicals for Attenuating Chemotherapeutic Drug-Induced Acute Kidney Injury

Zitong Zhu, Xinchen Liu, Penghui Li, Huan Wang, Yanjie Zhang, Mengmeng Liu and Jinsong Ren

ACS Appl. Mater. Interfaces, 2023, 15, 21854
DOI: 10.1021/acsami.3c00714

Unsaturated Phosphine Oxides for Modular Antibody Rebridging and Single Reagent Peptide‐Cyclization‐Bioconjugation

Christian E. Stieger, Alastair J. McMillan, Mark A. R. de Geus, Jan Vincent V. Arafiles, Luise Franz and Christian P. R. Hackenberger

Angew Chem Int Ed, 2025, 64
DOI: 10.1002/anie.202508656

Transglutaminase in Foods and Biotechnology

Katja Vasić, Željko Knez and Maja Leitgeb

IJMS, 2023, 24, 12402
DOI: 10.3390/ijms241512402

Exploration of the antibody–drug conjugate clinical landscape

Heather Maecker, Vidya Jonnalagadda, Sunil Bhakta, Vasu Jammalamadaka and Jagath R. Junutula

mAbs, 2023, 15
DOI: 10.1080/19420862.2023.2229101

Synthesis and Evaluation of Three Azide-Modified Disaccharide Oxazolines as Enzyme Substrates for Single-Step Fc Glycan-Mediated Antibody-Drug Conjugation

Xiao Zhang, Chong Ou, Huiying Liu and Lai-Xi Wang

Bioconjugate Chem., 2022, 33, 1179
DOI: 10.1021/acs.bioconjchem.2c00142

Catalytic Phosphorylation of Tyrosine via a Radical Arbuzov Reaction

Benjamin D. A. Shennan, Tomoyuki Fukuta, Mina Yamane, Takashi Koyama, Harunobu Mitsunuma and Motomu Kanai

J. Am. Chem. Soc., 2025, 147, 6349
DOI: 10.1021/jacs.4c17637

Fast and efficient cysteine-specific bioconjugation enables protein functionalization and rapid quantitative thiol reactivity profiling

Linfeng Chen, Jixiang He, Ziyi Wang, Tianyang Wang, Mengzhao Li, Huiling Wang, Changlin Liu, Jing Yang and Chunrong Liu

Sci. China Chem., 2026
DOI: 10.1007/s11426-025-3258-8

Recent Technological and Intellectual Property Trends in Antibody–Drug Conjugate Research

Youngbo Choi, Youbeen Choi and Surin Hong

Pharmaceutics, 2024, 16, 221
DOI: 10.3390/pharmaceutics16020221

Sensitive Immunofluorescent Detection of the PRAME Antigen Using a Practical Antibody Conjugation Approach

Ksenia A. Sapozhnikova, Vsevolod A. Misyurin, Dmitry Y. Ryazantsev, Egor A. Kokin, Yulia P. Finashutina, Anastasiya V. Alexeeva, Igor A. Ivanov, Milita V. Kocharovskaya, Nataliya A. Tikhonova, Galina P. Popova, Vera A. Alferova, Alexey V. Ustinov, Vladimir A. Korshun and Vladimir A. Brylev

IJMS, 2021, 22, 12845
DOI: 10.3390/ijms222312845

Selective Reduction of Cysteine Mutant Antibodies for Site-Specific Antibody–Drug Conjugates

Xiaoli Liao, Anthony Haight, Dennie Welch and Linjie Han

Bioconjugate Chem., 2023, 34, 2293
DOI: 10.1021/acs.bioconjchem.3c00425

Hypervalent Iodine Amino Acid Building Blocks for Bioorthogonal Peptide Macrocyclization

Xing‐Yu Liu, Olha Mykhailenko, Adriana Faraone and Jerome Waser

Angewandte Chemie, 2024, 136
DOI: 10.1002/ange.202404747

3-Methylpyrazole-Mediated C-Terminal Protein Modification

Xinyue Zhang and Chunmao He

Org. Lett., 2025, 27, 7451
DOI: 10.1021/acs.orglett.5c02315

Clinical Pharmacology of Antibody-Drug Conjugates

Iftekhar Mahmood

Antibodies, 2021, 10, 20
DOI: 10.3390/antib10020020

Site-Specific Antibody Conjugation with Payloads beyond Cytotoxins

Qun Zhou

Molecules, 2023, 28, 917
DOI: 10.3390/molecules28030917

Computational design of a single-chain galectin-1 yields a stable variant with retained glycan binding activity

Dajana Kolanovic, Markus Braun, Rajeev Pasupuleti, Georg Mlynek, Jakob Wallner, Gustav Oberdorfer and Birgit Wiltschi

Journal of Biotechnology, 2026, 414, 163
DOI: 10.1016/j.jbiotec.2026.03.011

Peptide‐Directed Attachment of Hydroxylamines to Specific Lysines of IgG Antibodies for Bioconjugations with Acylboronates

Matthias Tanriver, Marco Müller, Mikail D. Levasseur, Daniel Richards, Sohei Majima, Andrew DeMello, Yohei Yamauchi and Jeffrey W. Bode

Angew Chem Int Ed, 2024, 63
DOI: 10.1002/anie.202401080

ABNO‐Catalyzed Aerobic Oxidation of Thiols to Disulfides under Atmospheric Pressure

Zhiguang Zhang, Xiaojie Lan, Xiaomin Zhang, Yanmei Liu, Jinxin Gao, Bingzhu Zhang and Haixia Wu

Asian J Org Chem, 2023, 12
DOI: 10.1002/ajoc.202300009

Monoclonal War: The Antibody Arsenal and Targets for Expanded Application

Eric Rosenn, Mickael Benhaim, Allison Siegel, David Stein, Joseph Leonard, Erik Katcher, Dania Halperin and Zachary Mostel

Immuno, 2023, 3, 346
DOI: 10.3390/immuno3030021

Exploring the Sensitivity of Antibody–Drug Conjugate Efficacy to the Selection of Payload, Antibody, and Cell line

Mara Rao, Shruthi Murali, Danielle Amores, Feifan Yu and Andrew Tsourkas

Bioconjugate Chem., 2024, 35, 115
DOI: 10.1021/acs.bioconjchem.3c00537

Attenuated Toxicity and Antitoxic Mechanism via Sodium Iodide Symporter Inhibition-Based Tumor-Selective Delivery in Astatine-211 Radioimmunotherapy

Hiroki Takashima, Ryo Tsumura, Yoshikatsu Koga, Takahiro Anzai, Xiaojie Yin, Nozomi Sato, Yudai Shigekawa, Yousuke Kanayama, Akihiro Nambu, Sachiko Usuda, Hiromitsu Haba, Shingo Sakashita, Anri Inaki, Shino Manabe and Masahiro Yasunaga

Mol. Pharmaceutics, 2026, 23, 2422
DOI: 10.1021/acs.molpharmaceut.5c01438

Peptide and Protein Cysteine Modification Enabled by Hydrosulfuration of Ynamide

Changliu Wang, Zhenguang Zhao, Reem Ghadir, Dechun Yang, Zhenjia Zhang, Zhe Ding, Yuan Cao, Yuqing Li, Rosi Fassler, Dana Reichmann, Yujie Zhang, Yongli Zhao, Can Liu, Xiaobao Bi, Norman Metanis and Junfeng Zhao

ACS Cent. Sci., 2024, 10, 1742
DOI: 10.1021/acscentsci.4c01148

Engineering Pyrrolysine Systems for Genetic Code Expansion and Reprogramming

Daniel L. Dunkelmann and Jason W. Chin

Chem. Rev., 2024, 124, 11008
DOI: 10.1021/acs.chemrev.4c00243

Site-Selective Antibody Conjugation with Dibromopyrazines

Dénes Szepesi Kovács, Bettina Pásztor, Péter Ábrányi-Balogh, László Petri, Tímea Imre, József Simon, Enikő Tátrai, György Várady, József Tóvári, Peter A. Szijj and György M. Keserű

Bioconjugate Chem., 2024, 35, 1373
DOI: 10.1021/acs.bioconjchem.4c00296

Precision Labeling of Native Antibodies with Lock Coupling

Yazhi Liu, Isha Nadig, Abijeet Singh Mehta, Shih-Wei Chuo, Yen H. Ho, James Tyler, Charles S. Craik, Mekhail Anwar and Bruce E. Cohen

J. Am. Chem. Soc., 2026, 148, 2008
DOI: 10.1021/jacs.5c20725

Multiepitope recognition technology promotes the in-depth analysis of antibody‒drug conjugates

Yutian Lei, Yuan Shen, Feng Chen, Rui He, Zhang Zhang, Ying Zhou, Jin-Chen Yu, Jacques Crommen, Zhengjin Jiang and Qiqin Wang

Acta Pharmaceutica Sinica B, 2024, 14, 4962
DOI: 10.1016/j.apsb.2024.06.007

Recent progress of chemical methods for lysine site-selective modification of peptides and proteins

Jian Li, Jinjin Chen, Qi-Long Hu, Zhen Wang and Xiao-Feng Xiong

Chinese Chemical Letters, 2025, 36, 110126
DOI: 10.1016/j.cclet.2024.110126

An Ionic Liquid Medium Enables Development of a Phosphine-Mediated Amine–Azide Bioconjugation Method

Hisham M. El-Shaffey, Elizabeth J. Gross, Yvonne D. Hall and Jun Ohata

J. Am. Chem. Soc., 2021, 143, 12974
DOI: 10.1021/jacs.1c06092

A series of selective events

Ana Koperniku

Nat Rev Chem, 2021, 5, 674
DOI: 10.1038/s41570-021-00317-x

Enzymatic Construction of DARPin-Based Targeted Delivery Systems Using Protein Farnesyltransferase and a Capture and Release Strategy

Yi Zhang, Yiao Wang, Safak Uslu, Sneha Venkatachalapathy, Mohammad Rashidian, Jonas V. Schaefer, Andreas Plückthun and Mark D. Distefano

IJMS, 2022, 23, 11537
DOI: 10.3390/ijms231911537

Click Chemistry-Generated Auristatin F–Linker–Benzylguanine for a SNAP-Tag-Based Recombinant Antibody–Drug Conjugate Demonstrating Selective Cytotoxicity toward EGFR-Overexpressing Tumor Cells

Allan M. Huysamen, Olaolu E. Fadeyi, Grace Mayuni, Dennis M. Dogbey, Neelakshi Mungra, Fleury A. N. Biteghe, Natasha Hardcastle, Dharanidharan Ramamurthy, Olusiji A. Akinrinmade, Krupa Naran, Susan Cooper, Dirk Lang, Wolfgang Richter, Roger Hunter and Stefan Barth

ACS Omega, 2023, 8, 4026
DOI: 10.1021/acsomega.2c06844

A Review of Protein- and Peptide-Based Chemical Conjugates: Past, Present, and Future

Emily Holz, Martine Darwish, Devin B. Tesar and Whitney Shatz-Binder

Pharmaceutics, 2023, 15, 600
DOI: 10.3390/pharmaceutics15020600

The Journey of Antibody–Drug Conjugates: Lessons Learned from 40 Years of Development

Raffaele Colombo, Paolo Tarantino, Jamie R. Rich, Patricia M. LoRusso and Elisabeth G.E. de Vries

Cancer Discovery, 2024, 14, 2089
DOI: 10.1158/2159-8290.CD-24-0708

Anti-CD24 antibody-nitric oxide donor conjugates bearing a self-bioorthogonal cleavable linker

Jianbing Wu, Tianyue Cheng, Jiajun Xie, Ziyu Qian, Linhua Huang, Xun Yuan, Libang Zhang, Shan Yang, Yihua Zhang, Tonglin Xu, Juan Zhang and Zhangjian Huang

Acta Pharmaceutica Sinica B, 2025, 15, 5366
DOI: 10.1016/j.apsb.2025.07.037

Natural Product Based Antibody Drug Conjugates: Clinical Status as of November 9, 2020

David J. Newman

J. Nat. Prod., 2021, 84, 917
DOI: 10.1021/acs.jnatprod.1c00065

Glycosyltransferases as versatile tools to study the biology of glycans

Joshua M Kofsky, Jonathan L Babulic, Marie E Boddington, Fabiola V De León González and Chantelle J Capicciotti

Glycobiology, 2023, 33, 888
DOI: 10.1093/glycob/cwad092

Direct Preparation of Site‐Specific Antibody–Drug Conjugates with Unpurified Antibodies in Culture Medium

Mengru Lu, Yue Zeng, Jiaying Hang, Wei Shi, Wei Huang and Feng Tang

ChemBioChem, 2025, 26
DOI: 10.1002/cbic.202401082

Therapeutic peptides and proteins: Status and developments in drug delivery

Braxten D. Hornsby, Cheng Hua Lee, Cassidy A. Steele, Julius K.K. Tuekpe and Carol S. Lim

Journal of Controlled Release, 2026, 394, 114895
DOI: 10.1016/j.jconrel.2026.114895

Antibody drug conjugate: the “biological missile” for targeted cancer therapy

Zhiwen Fu, Shijun Li, Sifei Han, Chen Shi and Yu Zhang

Sig Transduct Target Ther, 2022, 7
DOI: 10.1038/s41392-022-00947-7

Site-Specific Chemoenzymatic Conjugation of High-Affinity M6P Glycan Ligands to Antibodies for Targeted Protein Degradation

Xiao Zhang, Huiying Liu, Jia He, Chong Ou, Thomas C. Donahue, Musleh M. Muthana, Lishan Su and Lai-Xi Wang

ACS Chem. Biol., 2022, 17, 3013
DOI: 10.1021/acschembio.1c00751

Catalyst‐ and Metal‐Free Photo‐Oxidative Coupling of Thiols with BrCCl3

Xiaoman Li, Jiali Fan, Dezhi Cui, Hui Yan, Shiquan Shan, Yongna Lu, Xiamin Cheng and Teck‐Peng Loh

Eur J Org Chem, 2022, 2022
DOI: 10.1002/ejoc.202200340

Antibody-Mediated Delivery of Chimeric BRD4 Degraders. Part 1: Exploration of Antibody Linker, Payload Loading, and Payload Molecular Properties

Peter S. Dragovich, Thomas H. Pillow, Robert A. Blake, Jack D. Sadowsky, Emel Adaligil, Pragya Adhikari, Sunil Bhakta, Nicole Blaquiere, Jinhua Chen, Josefa dela Cruz-Chuh, Karen E. Gascoigne, Steven J. Hartman, Mingtao He, Susan Kaufman, Tracy Kleinheinz, Katherine R. Kozak, Liang Liu, Liling Liu, Qi Liu, Ying Lu, Fanwei Meng, Melinda M. Mulvihill, Aimee O’Donohue, Rebecca K. Rowntree, Leanna R. Staben, Steven T. Staben, John Wai, Jian Wang, BinQing Wei, Catherine Wilson, Jianfeng Xin, Zijin Xu, Hui Yao, Donglu Zhang, Hongyan Zhang, Hao Zhou and Xiaoyu Zhu

J. Med. Chem., 2021, 64, 2534
DOI: 10.1021/acs.jmedchem.0c01845

Peptide‐Directed Attachment of Hydroxylamines to Specific Lysines of IgG Antibodies for Bioconjugations with Acylboronates

Matthias Tanriver, Marco Müller, Mikail D. Levasseur, Daniel Richards, Sohei Majima, Andrew DeMello, Yohei Yamauchi and Jeffrey W. Bode

Angewandte Chemie, 2024, 136
DOI: 10.1002/ange.202401080

Directed evolution of aminoacyl-tRNA synthetases through in vivo hypermutation

Yuichi Furuhata, Gordon Rix, James A. Van Deventer and Chang C. Liu

Nat Commun, 2025, 16
DOI: 10.1038/s41467-025-60120-w

‘Targeting’ Improved Outcomes with Antibody-Drug Conjugates in Non-Small Cell Lung Cancer—An Updated Review

Saurav Verma, Daniel Breadner and Jacques Raphael

Current Oncology, 2023, 30, 4329
DOI: 10.3390/curroncol30040330

Site‐ and Stereoselective Glycomodification of Biomolecules through Carbohydrate‐Promoted Pictet–Spengler Reaction

Bo Liu, Xiangman Zou, Yue Zhang, Yang Yang, Hao Xu, Feng Tang, Huixin Yu, Fei Xia, Zhi Liu, Jianwei Zhao, Wei Shi and Wei Huang

Angewandte Chemie, 2024, 136
DOI: 10.1002/ange.202401394

Enhancing Selectivity in Affinity Biosensors through Biorecognition-Driven Suppression of Nonspecific Binding

Yang Zhang, Feng Hu, Ruiyun Zhou, Tianxi Yang, Pengcheng Cai, Pierre Picchetti, Xiaowei Huang, Zhihua Li, Xiaodong Zhai, Roujia Zhang, Junjun Zhang, Jiyong Shi, Zhiming Guo, Shipeng Gao and Xiaobo Zou

ACS Sens., 2026, 11, 853
DOI: 10.1021/acssensors.5c03955

An intelligent cell-selective polymersome-DM1 nanotoxin toward triple negative breast cancer

Yifan Zhang, Shujing Yue, Rainer Haag, Huanli Sun and Zhiyuan Zhong

Journal of Controlled Release, 2021, 340, 331
DOI: 10.1016/j.jconrel.2021.11.014

Emerging biotechnologies for evaluating disruption of stress, sleep, and circadian rhythm mechanism using aptamer-based detection of salivary biomarkers

Meenakshi Pundir, Silvana Papagerakis, Maria C. De Rosa, Nikos Chronis, Katsuo Kurabayashi, Shahad Abdulmawjood, Mark Edward P. Prince, Liubov Lobanova, Xiongbiao Chen and Petros Papagerakis

Biotechnology Advances, 2022, 59, 107961
DOI: 10.1016/j.biotechadv.2022.107961

Genetic Code Expansion: Recent Developments and Emerging Applications

Yujia Huang, Pan Zhang, Haoyu Wang, Yan Chen, Tao Liu and Xiaozhou Luo

Chem. Rev., 2025, 125, 523
DOI: 10.1021/acs.chemrev.4c00216

Controlled Reversible N-Terminal Modification of Peptides and Proteins

Zeng Lin, Bo Liu, Mengru Lu, Yongqin Wang, Xuelian Ren, Zhaoxi Liu, Caili Luo, Wei Shi, Xiangman Zou, Xiaohan Song, Feng Tang, He Huang and Wei Huang

J. Am. Chem. Soc., 2024, 146, 23752
DOI: 10.1021/jacs.4c04894

A bispecific nanobody-drug conjugate targeting TROP2 and c-Met for low-concentration, single-dose treatment of pancreatic cancer

Wenjing Ning, Han Liu, Hongye Zeng, Xiaojing Qin, Lin Xu, Shiting Yang, Yue Wang, Fentian Chen, Na Yuan, Xiaoqing Chen, Tao Xu, Kexin Wu, Peng Wang, Chao Liu, Yuanzhi Chen, Ningshao Xia, Xue Liu and Wenxin Luo

Cell Reports Medicine, 2026, 102688
DOI: 10.1016/j.xcrm.2026.102688

Synthetic Site-Specific Antibody–Ligand Conjugates Promote Asialoglycoprotein Receptor-Mediated Degradation of Extracellular Human PCSK9

Thomas C. Donahue, Chong Ou, Qiang Yang, Robin Flinko, Xiao Zhang, Guanghui Zong, George K. Lewis and Lai-Xi Wang

ACS Chem. Biol., 2023, 18, 1611
DOI: 10.1021/acschembio.3c00229

Antibody-drug conjugates in cancer therapy: applications and future advances

Rou Long, Hanrong Zuo, Guiyang Tang, Chaohui Zhang, Xinru Yue, Jinsai Yang, Xinyu Luo, Yuqi Deng, Jieya Qiu, Jiale Li and Jianhong Zuo

Front. Immunol., 2025, 16
DOI: 10.3389/fimmu.2025.1516419

Facile Rebridging Conjugation Approach to Attain Monoclonal Antibody-Targeted Nanoparticles with Enhanced Antigen Binding and Payload Delivery

Bayan Alkhawaja, Duaa Abuarqoub, Mohammad Al-natour, Walhan Alshaer, Qasem Abdallah, Ezaldeen Esawi, Malak Jaber, Nour Alkhawaja, Bayan Y. Ghanim, Nidal Qinna and Andrew G. Watts

Bioconjugate Chem., 2024
DOI: 10.1021/acs.bioconjchem.4c00275

An Insight into FDA Approved Antibody-Drug Conjugates for Cancer Therapy

Juliana T. W. Tong, Paul W. R. Harris, Margaret A. Brimble and Iman Kavianinia

Molecules, 2021, 26, 5847
DOI: 10.3390/molecules26195847

A Combination of Native LC-MS Approaches for the Comprehensive Characterization of the Antibody-Drug Conjugate Trastuzumab Deruxtecan

Evolène Deslignière, Hélène Diemer, Stéphane Erb, Pierre Coliat, Xavier Pivot, Alexandre Detappe, Oscar Hernandez-Alba and Sarah Cianférani

Front. Biosci. (Landmark Ed), 2022, 27
DOI: 10.31083/j.fbl2710290

Chemotherapeutic Drug—Antibody Conjugates (ChemoBodies): Recent Advances and Future Directions

Abhishek K. Tiwatane, Prakash Y. Khandave, Sampada Sharad Kulkarni, Kounosuke Oisaki and Abhay H. Pande

Curr Oncol Rep, 2025, 27, 1287
DOI: 10.1007/s11912-025-01713-y

Hypervalent Iodine Amino Acid Building Blocks for Bioorthogonal Peptide Macrocyclization

Xing‐Yu Liu, Olha Mykhailenko, Adriana Faraone and Jerome Waser

Angew Chem Int Ed, 2024, 63
DOI: 10.1002/anie.202404747

Nickel-Catalyzed Antibody Bioconjugation

Vlad Bacauanu, Zoe N. Merz, Zhong L. Hua and Simon B. Lang

J. Am. Chem. Soc., 2023, 145, 25842
DOI: 10.1021/jacs.3c10185

Development of an E. coli strain for cell‐free ADC manufacturing

Dan Groff, Nina A. Carlos, Rishard Chen, Jeffrey A. Hanson, Shengwen Liang, Stephanie Armstrong, Xiaofan Li, Sihong Zhou, Alex Steiner, Trevor J. Hallam and Gang Yin

Biotech & Bioengineering, 2022, 119, 162
DOI: 10.1002/bit.27961

Application of a Biocatalytic Strategy for the Preparation of Tiancimycin-Based Antibody–Drug Conjugates Revealing Key Insights into Structure–Activity Relationships

Andrew D. Steele, Alexander F. Kiefer, Dobeen Hwang, Dong Yang, Christiana N. Teijaro, Ajeeth Adhikari, Christoph Rader and Ben Shen

J. Med. Chem., 2023, 66, 1562
DOI: 10.1021/acs.jmedchem.2c01771

Perspectives on the development of antibody-drug conjugates targeting ROR1 for hematological and solid cancers

Haiyong Peng

Antibody Therapeutics, 2021, 4, 222
DOI: 10.1093/abt/tbab023

Pd(I)-catalyzed ring-opening arylation of cyclopropyl-α-aminoamides: Access to α-ketoamide peptidomimetics

Yue Sun, Liming Yang, Yaohang Cheng, Guanghui An and Guangming Li

Chinese Chemical Letters, 2024, 35, 109250
DOI: 10.1016/j.cclet.2023.109250

Azobenzene‐Based Linker Strategy for Selective Activation of Antibody–Drug Conjugates

Dian Xiao, Lianqi Liu, Fei Xie, Jingwen Dong, Yanming Wang, Xin Xu, Wu Zhong, Hongbin Deng, Xinbo Zhou and Song Li

Angewandte Chemie, 2024, 136
DOI: 10.1002/ange.202310318

Site‐ and Stereoselective Glycomodification of Biomolecules through Carbohydrate‐Promoted Pictet–Spengler Reaction

Bo Liu, Xiangman Zou, Yue Zhang, Yang Yang, Hao Xu, Feng Tang, Huixin Yu, Fei Xia, Zhi Liu, Jianwei Zhao, Wei Shi and Wei Huang

Angew Chem Int Ed, 2024, 63
DOI: 10.1002/anie.202401394

ez-ADiCon: A novel glyco-remodeling based strategy that enables preparation of homogenous antibody-drug conjugates via one-step enzymatic transglycosylation with payload-preloaded bi-antennary glycan complexes

Hyongi Chon, Satoshi Kanamori, Kazuhiro Hibino, Takashi Nagahara, Tomohiko Suzuki, Keiichiro Ohara and Hideki Narumi

Bioorganic & Medicinal Chemistry Letters, 2023, 80, 129117
DOI: 10.1016/j.bmcl.2022.129117

Profiling of BCLxL Protein Complexes in Non-Small Cell Lung Cancer Cells via Multiplexed Single-Molecule Pull-Down and Co-Immunoprecipitation

Shi Ho Kim, Changju Chun and Tae-Young Yoon

Anal. Chem., 2024, 96, 8932
DOI: 10.1021/acs.analchem.3c05801

Diverse Transformations of MOFs Depending on the Structure of Thiol-Group Agents

Hang Xu, Yan Guo, Xu Wang, Shunsheng Ye, Liying Zhang, Tieqiang Wang, Yu Fu and Fuqiang Fan

Langmuir, 2025, 41, 31551
DOI: 10.1021/acs.langmuir.5c04684

General and Robust Chemoenzymatic Method for Glycan-Mediated Site-Specific Labeling and Conjugation of Antibodies: Facile Synthesis of Homogeneous Antibody–Drug Conjugates

Xiao Zhang, Chong Ou, Huiying Liu, Sunaina Kiran Prabhu, Chao Li, Qiang Yang and Lai-Xi Wang

ACS Chem. Biol., 2021, 16, 2502
DOI: 10.1021/acschembio.1c00597

Introduction of Reactive Thiol Handles into Tyrosine-Tagged Proteins through Enzymatic Oxidative Coupling

Paul Huang, Wendy Cao, Jennifer L. Fetzer, Nicholas S. Dolan and Matthew B. Francis

J. Am. Chem. Soc., 2025, 147, 23834
DOI: 10.1021/jacs.5c06195

Development of [177Lu]Lu-LNC1003 for radioligand therapy of prostate cancer with a moderate level of PSMA expression

Xuejun Wen, Pengfei Xu, Xinying Zeng, Jia Liu, Chao Du, Xueyuan Zeng, Xingxing Cheng, Xueqi Wang, Yuanyuan Liang, Tianzhi Zhao, Hongzhang Yang, Huifeng Li, Lingxin Meng, Jianyang Fang, Hongwu Liu, Zijian Zhou, Jingjing Zhang, Xianzhong Zhang, Zhide Guo and Xiaoyuan Chen

Eur J Nucl Med Mol Imaging, 2023, 50, 2846
DOI: 10.1007/s00259-023-06229-w

Broadening the Therapeutic Window of ADCs Using Site-Specific Bioconjugation Showcased by an MMAE-Containing Peptide Linker in a CD79b-Targeting ADC

Philipp Probst, Isabella Attinger-Toller, Romain Bertrand, Ramona Stark, Roger Santimaria, Bernd Schlereth, Dragan Grabulovski and Philipp René Spycher

Molecular Cancer Therapeutics, 2025, 24, 803
DOI: 10.1158/1535-7163.MCT-24-0983

Targeting antibodies dissociate from drug delivery liposomes during blood circulation

Unnur J. Björgvinsdóttir, Jannik B. Larsen, Martin Bak, Thomas L. Andresen and Rasmus Münter

Journal of Controlled Release, 2025, 379, 982
DOI: 10.1016/j.jconrel.2025.01.047

Towards Aptamer-Targeted Drug Delivery to Brain Tumors: The Synthesis of Ramified Conjugates of an EGFR-Specific Aptamer with MMAE on a Cathepsin B-Cleavable Linker

Vladimir A. Brylev, Ekaterina V. Ryabukhina, Ekaterina V. Nazarova, Nadezhda S. Samoylenkova, Evgeny L. Gulyak, Ksenia A. Sapozhnikova, Fatima M. Dzarieva, Alexey V. Ustinov, Igor N. Pronin, Dmitry Y. Usachev, Alexey M. Kopylov, Andrey V. Golovin, Galina V. Pavlova, Dmitry Yu. Ryazantsev and Vladimir A. Korshun

Pharmaceutics, 2024, 16, 1434
DOI: 10.3390/pharmaceutics16111434

SnoopLigase Enables Highly Efficient Generation of C–C-Linked Bispecific Nanobodies Targeting TNF-α and IL-17A

Jiewen Chen, Chundong Huang, Wei Zhao, Jun Ren, Fangling Ji and Lingyun Jia

Bioconjugate Chem., 2022, 33, 1446
DOI: 10.1021/acs.bioconjchem.2c00143

Trifunctional Dibromomaleimide Reagents Built Around A Lysine Scaffold Deliver Site‐selective Dual‐modality Antibody Conjugation

Yanbo Zhao, Vijay Chudasama and James R. Baker

ChemBioChem, 2023, 24
DOI: 10.1002/cbic.202300356

Noncanonical amino acids as doubly bio-orthogonal handles for one-pot preparation of protein multiconjugates

Yong Wang, Jingming Zhang, Boyang Han, Linzhi Tan, Wenkang Cai, Yuxuan Li, Yeyu Su, Yutong Yu, Xin Wang, Xiaojiang Duan, Haoyu Wang, Xiaomeng Shi, Jing Wang, Xing Yang and Tao Liu

Nat Commun, 2023, 14
DOI: 10.1038/s41467-023-36658-y

Understanding the Chemical Characteristics of Payloads and the Expression of Tumor-Associated Antigens of ADCs in Clinical Development

Cristina Nieto-Jiménez, Lucía Paniagua-Herranz, Carlo Bosi, Elisa Poyatos-Racionero, Manuel Pedregal, Víctor Moreno, Emiliano Calvo, Elena Domínguez-Jurado, Tatiana Hernández, Pedro Pérez-Segura, Balázs Győrffy, Carlos Alonso-Moreno, Giampaolo Bianchini and Alberto Ocana

ACS Omega, 2025, 10, 55126
DOI: 10.1021/acsomega.5c09181

Chemical Tagging of Bioactive Amides by Cooperative Catalysis: Applications in the Syntheses of Drug Conjugates

Cunyuan Zhao, Yuankai Wang, Quan Pham, Changhang Dai, Abhishek Chatterjee and Masayuki Wasa

J. Am. Chem. Soc., 2023, 145, 14233
DOI: 10.1021/jacs.3c00169

Chemical Modification of Peptides and Proteins Using Spirooxindole Oxirane Derivatives

Santosh S. Chavan, Hidetoshi Saze and Fujie Tanaka

Adv Synth Catal, 2023, 365, 2171
DOI: 10.1002/adsc.202300578

The Evolution of Antibody‐Drug Conjugates: Toward Accurate DAR and Multi‐specificity

Wenge Dong, Wanqi Wang and Chan Cao

ChemMedChem, 2024, 19
DOI: 10.1002/cmdc.202400109

Multilevel Characterization of a Chemoenzymatic Conjugated ADC by icIEF‐UV/MS and RP‐HPLC‐MS EAD Fragmentation Peptide Map

Scott Mack, Haichuan Liu, Erica Andersson and Yuzhuo Zhang

Electrophoresis, 2026, 47, 162
DOI: 10.1002/elps.70069

Biomimetic Carbon‐Based Nanomaterials: From Design Strategies to Next‐Generation Biosensing and Theranostic Applications

Marzieh Ramezani Farani, Ashkan Zandi, Fatemeh Shojaeian, Mingzhen Zhang, Danial Khorsandi, Fariba Mollarasouli, Iraj Alipourfard, Amin Farahani, Yu Jung Choi, Heemin Kang and Yun Suk Huh

Small, 2025, 21
DOI: 10.1002/smll.202502711

Click chemistry in the synthesis of antibody-drug conjugates

Rostyslav Dudchak, Magdalena Podolak, Serhii Holota, Olga Szewczyk-Roszczenko, Piotr Roszczenko, Anna Bielawska, Roman Lesyk and Krzysztof Bielawski

Bioorganic Chemistry, 2024, 143, 106982
DOI: 10.1016/j.bioorg.2023.106982

Copper assisted sequence-specific chemical protein conjugation at a single backbone amide

Mengzhun Guo, Kai Zhao, Liang Guo, Rui Zhou, Qiuju He, Kuan Lu, Tian Li, Dandan Liu, Jinfeng Chen, Jing Tang, Xin Fu, Jinyun Zhou, Bei Zheng, Samuel I. Mann, Yongdeng Zhang, Jing Huang, Bing Yang, Ting Zhou, Yingjie Lei and Bobo Dang

Nat Commun, 2023, 14
DOI: 10.1038/s41467-023-43753-7

Fast and Selective Cysteine Conjugation Using para-Quinone Methides

Ruimin Zhang, Bo Li, Liuli Dong, Zhaoliang Hu, Xue Li, Xueyu Yao, Jia Zheng, Aijun Lin, Shang Gao, Taijun Hang, Xiaoxing Wu and Qian Chu

Org. Lett., 2024, 26, 8951
DOI: 10.1021/acs.orglett.4c03452

Antibody-Drug Conjugates Containing Payloads from Marine Origin

Iván Cheng-Sánchez, Federico Moya-Utrera, Cristina Porras-Alcalá, Juan M. López-Romero and Francisco Sarabia

Marine Drugs, 2022, 20, 494
DOI: 10.3390/md20080494

Mechanisms of resistance to antibody-drug conjugates in breast cancer

Baris Cerci, Ozge Saatci, Mark Basik and Ozgur Sahin

Drug Resistance Updates, 2026, 85, 101353
DOI: 10.1016/j.drup.2026.101353

Bioconjugation Technology Selection during Early-Stage Development – A Strategy to Streamline IND and Manufacturing Timelines

Nina Hentzen, Abbas El Sahili, Julien Lescar, Chuan Fa Liu and Raphael Frey

JADC, 2023
DOI: 10.14229/jadc.2023.07.10.002

Elemental mass spectrometry imaging of biomolecules using metal-conjugated probes

Anthony Thai, Thomas E. Lockwood, Ioannis Kohilas, Rosemary J. Bergin, Andrew M. McDonagh and David P. Bishop

Nat Rev Chem, 2025, 9, 672
DOI: 10.1038/s41570-025-00749-9

Emerging Role of Bispecific Antibodies in Precision Medicine, Cancer and Modern Therapeutics

Muhammad Faisal Shahid and Samra Khan

Curr Oncol Rep, 2026, 28
DOI: 10.1007/s11912-026-01759-6

Spotlight on ideal target antigens and resistance in antibody-drug conjugates: Strategies for competitive advancement

Mingxia Jiang, Qiao Li and Binghe Xu

Drug Resistance Updates, 2024, 75, 101086
DOI: 10.1016/j.drup.2024.101086

Antibody-based cancer therapy

Rebecca S. Goydel and Christoph Rader

Oncogene, 2021, 40, 3655
DOI: 10.1038/s41388-021-01811-8

Diazaborines Are a Versatile Platform to Develop ROS‐Responsive Antibody Drug Conjugates**

João P. M. António, Joana Inês Carvalho, Ana S. André, Joana N. R. Dias, Sandra I. Aguiar, Hélio Faustino, Ricardo M. R. M. Lopes, Luis F. Veiros, Gonçalo J. L. Bernardes, Frederico A. da Silva and Pedro M. P. Gois

Angew Chem Int Ed, 2021, 60, 25914
DOI: 10.1002/anie.202109835

Click Chemistry and Radiochemistry: An Update

David Bauer, Mike A. Cornejo, Tran T. Hoang, Jason S. Lewis and Brian M. Zeglis

Bioconjugate Chem., 2023, 34, 1925
DOI: 10.1021/acs.bioconjchem.3c00286

8C7: A Fully Human Anti‐PTGFRN Monoclonal Antibody‐Drug Conjugate Inhibiting Tumour Growth of Mesothelioma and Paediatric Medulloblastoma Cell Lines

Jorge Marquez, Jianping Dong, Binbin Yue, Jun Hayashi, Chun Dong, Mitsuo Oshimura and Ginette Serrero

J Cellular Molecular Medi, 2025, 29
DOI: 10.1111/jcmm.70665

Bioorthogonal CRISPR/Cas9‐Drug Conjugate: A Combinatorial Nanomedicine Platform

Marcel Janis Beha, Joo‐Chan Kim, San Hae Im, Yunsu Kim, Seungju Yang, Juhee Lee, Yu Ri Nam, Haeshin Lee, Hee‐Sung Park and Hyun Jung Chung

Advanced Science, 2023, 10
DOI: 10.1002/advs.202302253

Antibody–drug conjugates: From oncological milestones to emerging non-oncological applications

Urvashi Yadav and Rajesh Kumar

International Immunopharmacology, 2026, 171, 116093
DOI: 10.1016/j.intimp.2025.116093

One-step synthesis of site-specific antibody–drug conjugates by reprograming IgG glycoengineering with LacNAc-based substrates

Wei Shi, Wanzhen Li, Jianxin Zhang, Tiehai Li, Yakai Song, Yue Zeng, Qian Dong, Zeng Lin, Likun Gong, Shuquan Fan, Feng Tang and Wei Huang

Acta Pharmaceutica Sinica B, 2022, 12, 2417
DOI: 10.1016/j.apsb.2021.12.013

Azobenzene‐Based Linker Strategy for Selective Activation of Antibody–Drug Conjugates

Dian Xiao, Lianqi Liu, Fei Xie, Jingwen Dong, Yanming Wang, Xin Xu, Wu Zhong, Hongbin Deng, Xinbo Zhou and Song Li

Angew Chem Int Ed, 2024, 63
DOI: 10.1002/anie.202310318

Multi-Attribute Monitoring Method for Process Development of Engineered Antibody for Site-Specific Conjugation

Alistair R. Hines, Matthew Edgeworth, Paul W. A. Devine, Samuel Shepherd, Nicholas Chatterton, Claire Turner, Kathryn S. Lilley, Xiaoyu Chen and Nicholas J. Bond

J. Am. Soc. Mass Spectrom., 2023, 34, 1330
DOI: 10.1021/jasms.3c00037

The Emergence of Oligonucleotide Building Blocks in the Multispecific Proximity-Inducing Drug Toolbox of Destruction

Kevin Xiao Tong Zhou and Katherine E. Bujold

ACS Chem. Biol., 2025, 20, 3
DOI: 10.1021/acschembio.4c00311

Chemically Enhanced Peptide and Protein Therapeutics

Cristina Díaz-Perlas and Benjamí Oller-Salvia

Pharmaceutics, 2023, 15, 827
DOI: 10.3390/pharmaceutics15030827

The Chemistry Behind ADCs

Vesela Kostova, Patrice Désos, Jérôme-Benoît Starck and Andras Kotschy

Pharmaceuticals, 2021, 14, 442
DOI: 10.3390/ph14050442

Development of Ts-Protected Selenocysteine for Sec-Conjugate Arylation via a Reductive Coupling Approach

Qinshuo Zhang, Shiang Zhai, Qingqing Lu, Shuai Cheng, Shiping Wang, Ruo Wang, Ying Liu and Chunfa Xu

Org. Lett., 2025, 27, 12543
DOI: 10.1021/acs.orglett.5c03945

Antibody–drug conjugates in cancer therapy: current landscape, challenges, and future directions

Bonan Chen, Xiaohong Zheng, Jialin Wu, Guoming Chen, Jun Yu, Yi Xu, William K. K. Wu, Gary M. K. Tse, Ka Fai To and Wei Kang

Mol Cancer, 2025, 24
DOI: 10.1186/s12943-025-02489-2

ADCdb: the database of antibody–drug conjugates

Liteng Shen, Xiuna Sun, Zhen Chen, Yu Guo, Zheyuan Shen, Yi Song, Wenxiu Xin, Haiying Ding, Xinyue Ma, Weiben Xu, Wanying Zhou, Jinxin Che, Lili Tan, Liangsheng Chen, Siqi Chen, Xiaowu Dong, Luo Fang and Feng Zhu

Nucleic Acids Research, 2024, 52, D1097
DOI: 10.1093/nar/gkad831

Antibody-drug conjugates targeting HER2 for the treatment of urothelial carcinoma: potential therapies for HER2-positive urothelial carcinoma

Chia-Hsien Shih, Yu-Hua Lin, Hao-Lun Luo and Wen-Wei Sung

Front. Pharmacol., 2024, 15
DOI: 10.3389/fphar.2024.1326296

Photocatalyzed elaboration of antibody-based bioconjugates

Marine Le Stum, Eugénie Romero and Gary A Molander

Beilstein J. Org. Chem., 2025, 21, 616
DOI: 10.3762/bjoc.21.49

Electrochemical labelling of hydroxyindoles with chemoselectivity for site-specific protein bioconjugation

Conor Loynd, Soumya Jyoti Singha Roy, Vincent J. Ovalle, Sarah E. Canarelli, Atanu Mondal, Delilah Jewel, Elise D. Ficaretta, Eranthie Weerapana and Abhishek Chatterjee

Nat. Chem., 2024, 16, 389
DOI: 10.1038/s41557-023-01375-y

Exatecan Antibody Drug Conjugates Based on a Hydrophilic Polysarcosine Drug-Linker Platform

Louise Conilh, Guy Fournet, Eric Fourmaux, Angélique Murcia, Eva-Laure Matera, Benoît Joseph, Charles Dumontet and Warren Viricel

Pharmaceuticals, 2021, 14, 247
DOI: 10.3390/ph14030247

Determination of the decapping efficiency of THIOMAB™ antibodies with the engineered cysteine in the Fc region for making antibody–drug conjugates by specific hinge fragmentation-liquid chromatography

Yun Yang, Jaymin M. Patel, Rong-Sheng Yang, Fengfei Ma, Xiangfeng Niu, Yixiao Zhang, Thomas Niedringhaus, Mohammad Al-Sayah and Xiaoyu Yang

Anal Bioanal Chem, 2025, 417, 847
DOI: 10.1007/s00216-024-05707-w

Research progress of antibody–drug conjugates in gynecologic cancer

Dongdong Xu, Zhe-Sheng Chen, Xuanwei Peng, Zhongqiu Lin and Huaiwu Lu

Holist Integ Oncol, 2024, 3
DOI: 10.1007/s44178-024-00114-8

Genetically Engineered Cellular Membrane Vesicles as Tailorable Shells for Therapeutics

En Ren, Chao Liu, Peng Lv, Junqing Wang and Gang Liu

Advanced Science, 2021, 8
DOI: 10.1002/advs.202100460

Diazaborines Are a Versatile Platform to Develop ROS‐Responsive Antibody Drug Conjugates**

João P. M. António, Joana Inês Carvalho, Ana S. André, Joana N. R. Dias, Sandra I. Aguiar, Hélio Faustino, Ricardo M. R. M. Lopes, Luis F. Veiros, Gonçalo J. L. Bernardes, Frederico A. da Silva and Pedro M. P. Gois

Angewandte Chemie, 2021, 133, 26118
DOI: 10.1002/ange.202109835

T cell receptor-directed antibody-drug conjugates for the treatment of T cell-derived cancers

Katrin Schoenfeld, Jan Habermann, Philipp Wendel, Julia Harwardt, Evelyn Ullrich and Harald Kolmar

Molecular Therapy: Oncology, 2024, 32, 200850
DOI: 10.1016/j.omton.2024.200850

In Vivo Comparison of Site-Specific and Site-Selective Methods for Pretargeted Imaging in a Murine Model of Colorectal Cancer

Merlin Zabrocki, Samantha Delaney, Lars Hvass, Umberto Maria Battisti, Andreas Kjær and Matthias M. Herth

Mol. Pharmaceutics, 2026, 23, 2089
DOI: 10.1021/acs.molpharmaceut.5c01802

Single Mutation on Trastuzumab Modulates the Stability of Antibody–Drug Conjugates Built Using Acetal-Based Linkers and Thiol-Maleimide Chemistry

Xhenti Ferhati, Ester Jiménez-Moreno, Emily A. Hoyt, Giulia Salluce, Mar Cabeza-Cabrerizo, Claudio D. Navo, Ismael Compañón, Padma Akkapeddi, Maria J. Matos, Noelia Salaverri, Pablo Garrido, Alfredo Martínez, Víctor Laserna, Thomas V. Murray, Gonzalo Jiménez-Osés, Peter Ravn, Gonçalo J. L. Bernardes and Francisco Corzana

J. Am. Chem. Soc., 2022, 144, 5284
DOI: 10.1021/jacs.1c07675

Antibody polymer drug conjugates with increased drug to antibody ratio: CD38-targeting nanomedicines for innovative therapy of relapsed lymphomas

Ondřej Lidický, Nicol Renešová, Júlia Kudláčová, Marcela Filipová, Tereza Běláková, Petra Kovaříková, Dmitry Manakov, Jan Pankrác, Alexandra Dolníková, Eva Pokorná, Pavel Klener and Tomáš Etrych

Journal of Controlled Release, 2025, 384, 113876
DOI: 10.1016/j.jconrel.2025.113876

Antibody-drug conjugates for the treatment of lymphoma: clinical advances and latest progress

Yurou Chu, Xiangxiang Zhou and Xin Wang

J Hematol Oncol, 2021, 14
DOI: 10.1186/s13045-021-01097-z

Late-Stage Desulfurization Enables Rapid and Efficient Solid-Phase Synthesis of Cathepsin-Cleavable Linkers for Antibody–Drug Conjugates

Marzieh Ahangarpour, Margaret A. Brimble and Iman Kavianinia

Bioconjugate Chem., 2024, 35, 1007
DOI: 10.1021/acs.bioconjchem.4c00199

Development of catalyst-free carbon-sulfur bond formation reactions under aqueous media and their applications

Min Sun Kang, Joycelyn Yi Xin Khoo, Zhenhua Jia and Teck-Peng Loh

Green Synthesis and Catalysis, 2022, 3, 309
DOI: 10.1016/j.gresc.2022.09.002

Importance and Considerations of Antibody Engineering in Antibody-Drug Conjugates Development from a Clinical Pharmacologist’s Perspective

Andrew T. Lucas, Amber Moody, Allison N. Schorzman and William C. Zamboni

Antibodies, 2021, 10, 30
DOI: 10.3390/antib10030030

Ferrocenyl Compounds as Alternative Redox Labels for Robust and Versatile Electrochemical Aptamer-Based Sensors

Gyeongho Kim, Soo Eun Park, Woohyeong Lee, Jung Min Joo and Haesik Yang

ACS Sens., 2024, 9, 6450
DOI: 10.1021/acssensors.4c01773

The BASHY Platform Enables the Assembly of a Fluorescent Bortezomib–GV1001 Conjugate

Silvia Baldo, Patrícia Antunes, João Falcão Felicidade, Fábio M. F. Santos, Jesús F. Arteaga, Fábio Fernandes, Uwe Pischel, Sandra N. Pinto and Pedro M. P. Gois

ACS Med. Chem. Lett., 2022, 13, 128
DOI: 10.1021/acsmedchemlett.1c00615

Enzymatic Bioconjugation: A Perspective from the Pharmaceutical Industry

Aaron Debon, Elina Siirola and Radka Snajdrova

JACS Au, 2023, 3, 1267
DOI: 10.1021/jacsau.2c00617

Conjugation Chemistry Markedly Impacts Toxicity and Biodistribution of Targeted Nanoparticles, Mediated by Complement Activation

Michael H. Zaleski, Liam S. Chase, Elizabeth D. Hood, Zhicheng Wang, Jia Nong, Carolann L. Espy, Marco E. Zamora, Jichuan Wu, Lianne J. Morrell, Vladimir R. Muzykantov, Jacob W. Myerson and Jacob S. Brenner

Advanced Materials, 2025, 37
DOI: 10.1002/adma.202409945

Quantifying antibody binding: techniques and therapeutic implications

James Lodge, Lewis Kajtar, Rachel Duxbury, David Hall, Glenn A. Burley, Joanna Cordy, James W.T. Yates and Zahra Rattray

mAbs, 2025, 17
DOI: 10.1080/19420862.2025.2459795

One-Pot Conversion of Free Sialoglycans to Functionalized Glycan Oxazolines and Efficient Synthesis of Homogeneous Antibody–Drug Conjugates through Site-Specific Chemoenzymatic Glycan Remodeling

Chong Ou, Chao Li, Roushu Zhang, Qiang Yang, Guanghui Zong, Yuanwei Dai, Rebecca L. Francis, Stylianos Bournazos, Jeffrey V. Ravetch and Lai-Xi Wang

Bioconjugate Chem., 2021, 32, 1888
DOI: 10.1021/acs.bioconjchem.1c00314

An Efficient Opal‐Suppressor Tryptophanyl Pair Creates New Routes for Simultaneously Incorporating up to Three Distinct Noncanonical Amino Acids into Proteins in Mammalian Cells**

Arianna O. Osgood, Yunan Zheng, Soumya Jyoti Singha Roy, Nikolaos Biris, Myer Hussain, Conor Loynd, Delilah Jewel, James S. Italia and Abhishek Chatterjee

Angewandte Chemie, 2023, 135
DOI: 10.1002/ange.202219269

Harnessing computational technologies to facilitate antibody–drug conjugate development

Anastasia Croitoru, Asuka A. Orr and Alexander D. MacKerell

Nat Chem Biol, 2025, 21, 1138
DOI: 10.1038/s41589-025-01950-z

Site-Specific Labeling of PD-L1 Fab through Disulfide Rebridging for ImmunoPET Imaging

Jiyao Yu, Charles Yen, Qunfeng Fu, Sheng-Yao Dai, Melwin Cheng and Jianghong Rao

Chemical & Biomedical Imaging, 2026
DOI: 10.1021/cbmi.6c00022

Theranostic antibody conjugates: A review of recent trends and applications in cancer

Keyvan Kheyrolahzadeh, Maryam Mojahedi, Mohammad Reza Tohidkia and Ayuob Aghanejad

Bioorganic Chemistry, 2025, 164, 108915
DOI: 10.1016/j.bioorg.2025.108915

Probing the Internalization and Efficacy of Antibody‐Drug Conjugate via Site‐Specific Fc‐Glycan Labelling of a Homogeneous Antibody Targeting SSEA‐4 Bearing Tumors

Vidya S Shivatare, Han‐Wen Huang, Tzu‐Hao Tseng, Po‐Kai Chuang, Yi‐Fang Zeng and Chi‐Huey Wong

Israel Journal of Chemistry, 2023, 63
DOI: 10.1002/ijch.202300042

Applications of genetic code expansion technology in eukaryotes

Qiao-ru Guo and Yu J Cao

Protein & Cell, 2024, 15, 331
DOI: 10.1093/procel/pwad051

Antibody drug conjugates in the clinic

Edidiong Udofa, Disha Sankholkar, Samir Mitragotri and Zongmin Zhao

Bioengineering & Transla Med, 2024, 9
DOI: 10.1002/btm2.10677

Antibody–Drug Conjugate Stability Probed by Variable-Temperature Electrospray Ionization Mass Spectrometry

Jan Fiala, Dina Schuster and Albert J. R. Heck

J. Am. Soc. Mass Spectrom., 2025, 36, 1395
DOI: 10.1021/jasms.5c00109

Repurposing organic semiconducting nanomaterials to accelerate clinical translation of NIR-II fluorescence imaging

Xiaoming Hu, Fengwei Sun, Caijun Zhu, Zhen Yang and Wei Huang

Nano Res., 2023, 16, 5140
DOI: 10.1007/s12274-022-5145-1

Conjugated therapeutic proteins as a treatment for bacteria which trigger cancer development

Mohamed Halawa, Precious M. Newman, Tope Aderibigbe and Valerie J. Carabetta

iScience, 2024, 27, 111029
DOI: 10.1016/j.isci.2024.111029

Harold Nathan Tan, Marta Ascanio Morcillo, Juanita Lopez, Anna Minchom, Adam Sharp, Alec Paschalis, Georgina Silva-Fortes, Bindu Raobaikady and Udai Banerji

J Hematol Oncol, 2025, 18
DOI: 10.1186/s13045-025-01720-3

Antibody–Drug Conjugates as an Emerging Therapy in Oncodermatology

Clara Esnault, David Schrama, Roland Houben, Serge Guyétant, Audrey Desgranges, Camille Martin, Patricia Berthon, Marie-Claude Viaud-Massuard, Antoine Touzé, Thibault Kervarrec and Mahtab Samimi

Cancers, 2022, 14, 778
DOI: 10.3390/cancers14030778

Strategies for the enhancement of anti-cancer effect of phosphodiesterase type 5 inhibitors using drug binding fusion proteins

Hongbin Kim, Chang Yeop Keum, Su Yeon Lim and Kwang Suk Lim

Biotechnol Bioproc E, 2024, 29, 85
DOI: 10.1007/s12257-024-00014-8

Development of applicable thiol-linked antibody–drug conjugates with improved stability and therapeutic index

Yanming Wang, Fei Xie, Lianqi Liu, Xin Xu, Shiyong Fan, Wu Zhong and Xinbo Zhou

Drug Delivery, 2022, 29, 754
DOI: 10.1080/10717544.2022.2039807

Antibody-drug conjugates in oncology: A spotlight on overcoming resistance

Xiaoxiao Xu, Tong Yu and Zhenxing Wang

Critical Reviews in Oncology/Hematology, 2026, 217, 105015
DOI: 10.1016/j.critrevonc.2025.105015

A Cost-Effective Pichia pastoris Cell-Free System Driven by Glycolytic Intermediates Enables the Production of Complex Eukaryotic Proteins

Jeffrey L. Schloßhauer, Srujan Kumar Dondapati, Stefan Kubick and Anne Zemella

Bioengineering, 2024, 11, 92
DOI: 10.3390/bioengineering11010092

Facile Generation of Heterotelechelic Poly(2‐Oxazoline)s Towards Accelerated Exploration of Poly(2‐Oxazoline)‐Based Nanomedicine

Joachim F. R. Van Guyse, Saed Abbasi, Kazuko Toh, Zlata Nagorna, Junjie Li, Anjaneyulu Dirisala, Sabina Quader, Satoshi Uchida and Kazunori Kataoka

Angew Chem Int Ed, 2024, 63
DOI: 10.1002/anie.202404972

Development and approval of novel injectables: enhancing therapeutic innovations

Pooja Yadav, Yuvraj Singh, Divya Chauhan, Pavan K. Yadav, Ashwini S. Kedar, Amrendra K. Tiwari, Aarti Abhishek Shah, Jiaur R. Gayen and Manish K. Chourasia

Expert Opinion on Drug Delivery, 2024, 21, 639
DOI: 10.1080/17425247.2024.2351987

High-Throughput Screening of Photo-Cross-Linking Peptide Libraries for Site-Specific Conjugation of IgG

Sangwoo Lee, Jisoo Park, Byoung Jun Lee, Jeonghyun Lee, Byoung Joon Ko, Eunha Kim and Tae Hyeon Yoo

Bioconjugate Chem., 2025, 36, 2655
DOI: 10.1021/acs.bioconjchem.5c00487

Engineering AND-Gate Aptamer-Signal Base Conjugates for Targeted Magnetic Resonance Molecular Imaging of Metastatic Cancer

Yazhou Li, Ting Li, Hong Chen, Linlin Wang, Yinghao Xia, Lili Zhang, Yuqi Xie, Jili Li, Can Luo, Yingjie Xu, Yanlan Liu and Weihong Tan

ACS Appl. Mater. Interfaces, 2022, 14, 17032
DOI: 10.1021/acsami.1c24048

An Antibody‐Drug Conjugate for Multiple Myeloma Prepared by Multi‐Arm Linkers

Yueh‐Hsiang Yu, Wei‐Ting Tian, Cédric Grauffel, Wei‐Chen Lin, Ming‐Yu Hsieh, Pei‐Wen Wu, Hui‐Ju Lee, Chi‐Jiun Peng, Pei‐Hsuan Lin, Hsing‐Mao Chu, Carmay Lim and Tse Wen Chang

Advanced Science, 2024, 11
DOI: 10.1002/advs.202307852

A comprehensive review of key factors affecting the efficacy of antibody drug conjugate

Anupama Samantasinghar, Naina Pullarkat Sunildutt, Faheem Ahmed, Afaque Manzoor Soomro, Abdul Rahim Chethikkattuveli Salih, Pratibha Parihar, Fida Hussain Memon, Kyung Hwan Kim, In Suk Kang and Kyung Hyun Choi

Biomedicine & Pharmacotherapy, 2023, 161, 114408
DOI: 10.1016/j.biopha.2023.114408

MIB guides: [89Zr]Zr-DFO-trastuzumab and [64Cu]Cu-NOTA-Trastuzumab for Preclinical Cancer Imaging

Cristina Simó, Alexander C. Vanover, E. Carmen Azevedo and Patrícia M. R. Pereira

Mol Imaging Biol, 2025, 27, 506
DOI: 10.1007/s11307-025-02022-3

N-Vinyl Acrylamides: Versatile Heterobifunctional Electrophiles for Thiol–Thiol Bioconjugations

Marzieh Ahangarpour, Iman Kavianinia, Paul A. Hume, Paul W. R. Harris and Margaret A. Brimble

J. Am. Chem. Soc., 2022, 144, 13652
DOI: 10.1021/jacs.2c04146

G protein-coupled receptor-targeting antibody-drug conjugates: Current status and future directions

Peyton High and Kendra S. Carmon

Cancer Letters, 2023, 564, 216191
DOI: 10.1016/j.canlet.2023.216191

The Nitrile Bis-Thiol Bioconjugation Reaction

Mikesh Patel, Nafsika Forte, Charlie R. Bishop, Michael J. Porter, Matthew Dagwell, Kersti Karu, Vijay Chudasama and James R. Baker

J. Am. Chem. Soc., 2024, 146, 274
DOI: 10.1021/jacs.3c08762

Revisiting Disulfide–Yne and Disulfide–Diazonium Reactions for Potential Direct Modification of Disulfide Bonds in Proteins

Wei-Cheng Hung, Cheng-Hao Jhang, Shou-Lin Weng, Chiu-Chun Chou, Chein-Hung Chen, Jung-Lee Lin and Jim-Min Fang

J. Org. Chem., 2022, 87, 9875
DOI: 10.1021/acs.joc.2c00903

Progress on Phage Display Technology: Tailoring Antibodies for Cancer Immunotherapy

Renato Kaylan Alves França, Igor Cabral Studart, Marcus Rafael Lobo Bezerra, Larissa Queiroz Pontes, Antonio Marcos Aires Barbosa, Marcelo Macedo Brigido, Gilvan Pessoa Furtado and Andréa Queiroz Maranhão

Viruses, 2023, 15, 1903
DOI: 10.3390/v15091903

Lot-to-Lot Variance in Immunoassays—Causes, Consequences, and Solutions

Yunyun Luo, Martin Pehrsson, Lasse Langholm, Morten Karsdal, Anne-Christine Bay-Jensen and Shu Sun

Diagnostics, 2023, 13, 1835
DOI: 10.3390/diagnostics13111835

Efficient Preparation of Homogenous Antibody Conjugates via Glycosite‐Specific Transglycosylation Enabled by Readily Available Glycosyl Donors

Deqin Cai, Yuan Zhao, Gaoyuan Lu, Chunrong Li, Yichong Lao, Ramesh Mudududdla, Jiahao Zhang, Peijing Jia, Penghsuan Huang, Wenxin Wu, Thao‐Vy T. Nguyen, Xuhui Huang, Lingjun Li and Weiping Tang

Angewandte Chemie, 2026, 138
DOI: 10.1002/ange.202518579

From concept to clinic: Cutting-Edge advances steering the next wave of antibody–drug conjugates innovation

Imsha Parveen, Anjlina Aqil, Sumit Sharma, Abdul Qadir, Sayed Abdur Rehman, Ashif Iqubal, Khang Wen Goh, Rajath Govind, Mohammad Kashif Iqubal and Prashant Kesharwani

Journal of Drug Delivery Science and Technology, 2026, 120, 108271
DOI: 10.1016/j.jddst.2026.108271

Production of antibodies and antibody fragments containing non-natural amino acids in Escherichia coli

Jacquelyn Blake-Hedges, Dan Groff, Wilson Foo, Jeffrey Hanson, Elenor Castillo, Miao Wen, Diana Cheung, Mary Rose Masikat, Jian Lu, Young Park, Nina Abi Carlos, Hans Usman, Kevin Fong, Abigail Yu, Sihong Zhou, Joyce Kwong, Cuong Tran, Xiaofan Li, Dawei Yuan, Trevor Hallam and Gang Yin

mAbs, 2024, 16
DOI: 10.1080/19420862.2024.2316872

Achieving cysteine-selective peptide/protein bioconjugation via tunable triazine-pyridine chemistry

Chaoming Wang, Ruijuan Yin, Hao Jiang, Qinbo Ma, Hongli Zhang, Shanyue Zheng, Rilei Yu, Han Liu, Xuechen Li and Tao Jiang

Sci. Adv., 2025, 11
DOI: 10.1126/sciadv.aea6904

Recent advances in biosynthesis of non-canonical amino acids and their potentials in strain engineering

Zhen Hou, Junkai Tuo, Xiaoyan Ma and Yi-Xin Huo

Results in Engineering, 2025, 25, 103641
DOI: 10.1016/j.rineng.2024.103641

A mild phenoxysilyl linker for self-immolative release of antibody-drug conjugates

Ding Wei, Yurong Mao, Huihui Wang, Siqi Qu, Jiakang Chen, Jiusheng Li, Biao Jiang and Hongli Chen

Chinese Chemical Letters, 2023, 34, 108091
DOI: 10.1016/j.cclet.2022.108091

Albubody: an engineered scFv variant platform for site-specific drug conjugation and enhanced tumor efficacy

Na Hyun Kwon, Jae Hun Lee, Yeongchae Kim, Young S. Hahn and Inchan Kwon

Journal of Controlled Release, 2025, 386, 114165
DOI: 10.1016/j.jconrel.2025.114165

Peptide-Drug Conjugates: A New Hope for Cancer Management

Vivek P. Chavda, Hetvi K. Solanki, Majid Davidson, Vasso Apostolopoulos and Joanna Bojarska

Molecules, 2022, 27, 7232
DOI: 10.3390/molecules27217232

More than Toxins—Current Prospects in Designing the Next Generation of Antibody Drug Conjugates

Jonathan Schwach, Mustafa Abdellatif and Andreas Stengl

Front. Biosci. (Landmark Ed), 2022, 27
DOI: 10.31083/j.fbl2708240

Evolution of Pyrrolysyl-tRNA Synthetase: From Methanogenesis to Genetic Code Expansion

Nikolaj G. Koch and Nediljko Budisa

Chem. Rev., 2024, 124, 9580
DOI: 10.1021/acs.chemrev.4c00031

Understanding the Effects of Site-Specific Light Chain Conjugation on Antibody Structure Using Hydrogen Exchange-Mass Spectrometry (HX-MS)

Sachini P. Karunaratne, Ehab M. Moussa, Brittney J. Mills and David D. Weis

Journal of Pharmaceutical Sciences, 2024, 113, 2065
DOI: 10.1016/j.xphs.2024.05.008

Preparation of porphyrin and phthalocyanine conjugates for biomedical applications

Iris Pontón and David Sánchez-García

J. Porphyrins Phthalocyanines, 2021, 25, 917
DOI: 10.1142/S1088424621300068

A Catalyst-Free, Tyrosine-Selective Bioconjugation Strategy via Triazine-Pyridine Chemistry for Antibodies

Shanyue Zheng, Chaoming Wang, Yifan Wang, Ruijuan Yin, Rilei Yu, Lu Liu, Hao Jiang, Xuechen Li and Tao Jiang

Org. Lett., 2026, 28, 3862
DOI: 10.1021/acs.orglett.6c00680

Advancements in site-specific modification of peptides based on the chemical reactivity of native amino acids

Ruiyao E, Wangsheng Sun and Rui Wang

Sci. Sin.-Chim, 2025, 55, 2180
DOI: 10.1360/SSC-2025-0050

Scope of Microbial Transglutaminase for Site-Specific and Oriented Immobilization of Native Antibodies from Various Host Species

Emily Beitello, Kwame Osei, Faith E. Breausche, Jon A. Friesen and Jeremy D. Driskell

Langmuir, 2026, 42, 6903
DOI: 10.1021/acs.langmuir.5c06485

CMC Regulatory Considerations for Antibody-Drug Conjugates

Karoline Bechtold-Peters, Andrea Ruggiero, Nienke Vriezen, Nathan Ihle, Armin Klein, Charles Morgan, Daniel Schweizer, Dengfeng Liu, Fred Jacobson, Jakob Buecheler, Mark Panek, Naomi Duggan, Padma Malyala, Philippe Dupraz, Priyanka Desai, Shufang Niu, Yiqing Feng and Xiangyang Wang

Journal of Pharmaceutical Sciences, 2023, 112, 2965
DOI: 10.1016/j.xphs.2023.09.007

Modular Chemical Construction of IgG-like Mono- and Bispecific Synthetic Antibodies (SynAbs)

Fabien Thoreau, Peter A. Szijj, Michelle K. Greene, Léa N. C. Rochet, Ioanna A. Thanasi, Jaine K. Blayney, Antoine Maruani, James R. Baker, Christopher J. Scott and Vijay Chudasama

ACS Cent. Sci., 2023, 9, 476
DOI: 10.1021/acscentsci.2c01437

Antibody–Calixarene Drug Conjugate: A General Drug Delivery Platform for Tumor-Targeted Therapy

Xueyao Wu, Shunyu Yao, Qingqing Huang, Ankang Ying, Qiushi Li, Xianghui Cao, Chun Wang, Jian Xiao, Nana Feng, Zhanzhan Zhang, Dongsheng Guo and Yang liu

ACS Appl. Mater. Interfaces, 2024, 16, 41939
DOI: 10.1021/acsami.4c09588

Development of small molecule–drug conjugates based on derivatives of natural proteasome inhibitors that exhibit selectivity for PSMA-expressing cancer cells

Takahiro Obara, Nanami Kawano, Kengo Tatsumi, Akira Katsuyama, Kohei Nakajima, Mikako Ogawa and Satoshi Ichikawa

Bioorganic & Medicinal Chemistry, 2024, 108, 117773
DOI: 10.1016/j.bmc.2024.117773

N-Azidoacetylglucosamine (GlcNAz)-Derived Sugar Oxazolines as a New Class of Substrates for Chemoenzymatic Site-Specific Antibody Bioconjugation

Guanghui Zong, Margaryta Gomozkova, Tala Azzam, Eric J. Sundberg and Lai-Xi Wang

JACS Au, 2026, 6, 1914
DOI: 10.1021/jacsau.5c01772

Is antibody-drug conjugate a rising star for clinical treatment of solid tumors? A systematic review and meta-analysis

Leyin Zhang, Deyi Shen, Lulin Yu, Yici Yan, Harpreet S. Wasan, Jieru Yu, Shuo Zhang and Leitao Sun

Critical Reviews in Oncology/Hematology, 2022, 177, 103758
DOI: 10.1016/j.critrevonc.2022.103758

Trastuzumab deruxtecan in breast cancer

Miguel Martín, Atanasio Pandiella, Emilio Vargas-Castrillón, Elena Díaz-Rodríguez, Teresa Iglesias-Hernangómez, Concha Martínez Cano, Inés Fernández-Cuesta, Elena Winkow and Maria Francesca Perelló

Critical Reviews in Oncology/Hematology, 2024, 198, 104355
DOI: 10.1016/j.critrevonc.2024.104355

Chemical Site-Specific Conjugation Platform to Improve the Pharmacokinetics and Therapeutic Index of Antibody–Drug Conjugates

Yutaka Matsuda, Takuya Seki, Kei Yamada, Yuri Ooba, Kazutoshi Takahashi, Tomohiro Fujii, Sayaka Kawaguchi, Takahiro Narita, Akira Nakayama, Yoshiro Kitahara, Brian A. Mendelsohn and Tatsuya Okuzumi

Mol. Pharmaceutics, 2021, 18, 4058
DOI: 10.1021/acs.molpharmaceut.1c00473

Protein Chemical Modification Using Highly Reactive Species and Spatial Control of Catalytic Reactions

Shinichi Sato

Chem. Pharm. Bull., 2022, 70, 95
DOI: 10.1248/cpb.c21-00915

Self‐Assembled L–DNA Linkers for Rapid Construction of Multi‐Specific Antibody‐Drug Conjugates Library

Liujuan Zhou, Fan Yang, Zhaoshuai Bai, Xiaohui Zhou, Zhihai Zhang, Zhihang Li, Junyuan Gong, Junqi Yu, Liqiang Pan, Chan Cao and James J. Chou

Angewandte Chemie, 2023, 135
DOI: 10.1002/ange.202302805

Thio-NHS esters are non-innocent protein acylating reagents

Weibing Liu, Aziz Khan, Yana Demyanenko, Shabaz Mohammed and Benjamin G. Davis

Nat Commun, 2025, 16
DOI: 10.1038/s41467-025-60527-5

The Evolving Landscape of Antibody–Drug Conjugates: In Depth Analysis of Recent Research Progress

Janet M. Sasso, Rumiana Tenchov, Robert Bird, Kavita A. Iyer, Krittika Ralhan, Yacidzohara Rodriguez and Qiongqiong Angela Zhou

Bioconjugate Chem., 2023, 34, 1951
DOI: 10.1021/acs.bioconjchem.3c00374

Facile Generation of Heterotelechelic Poly(2‐Oxazoline)s Towards Accelerated Exploration of Poly(2‐Oxazoline)‐Based Nanomedicine

Joachim F. R. Van Guyse, Saed Abbasi, Kazuko Toh, Zlata Nagorna, Junjie Li, Anjaneyulu Dirisala, Sabina Quader, Satoshi Uchida and Kazunori Kataoka

Angewandte Chemie, 2024, 136
DOI: 10.1002/ange.202404972

Advanced Antibody–Drug Conjugates Design: Innovation in Linker Chemistry and Site‐Specific Conjugation Technologies

Yutaka Matsuda, Jenny R. Chang and Brian A. Mendelsohn

ChemBioChem, 2025, 26
DOI: 10.1002/cbic.202500305

The Dawn of a New Era: Targeting the “Undruggables” with Antibody-Based Therapeutics

Linghui Qian, Xuefen Lin, Xue Gao, Rizwan Ullah Khan, Jia-Yu Liao, Shubo Du, Jingyan Ge, Su Zeng and Shao Q. Yao

Chem. Rev., 2023, 123, 7782
DOI: 10.1021/acs.chemrev.2c00915

Trends in the Development of Antibody-Drug Conjugates for Cancer Therapy

Chi Hun Song, Minchan Jeong, Hyukmin In, Ji Hoe Kim, Chih-Wei Lin and Kyung Ho Han

Antibodies, 2023, 12, 72
DOI: 10.3390/antib12040072

Efficient Preparation of Homogenous Antibody Conjugates via Glycosite‐Specific Transglycosylation Enabled by Readily Available Glycosyl Donors

Deqin Cai, Yuan Zhao, Gaoyuan Lu, Chunrong Li, Yichong Lao, Ramesh Mudududdla, Jiahao Zhang, Peijing Jia, Penghsuan Huang, Wenxin Wu, Thao‐Vy T. Nguyen, Xuhui Huang, Lingjun Li and Weiping Tang

Angew Chem Int Ed, 2026, 65
DOI: 10.1002/anie.202518579

Machine Learning for Predicting the Drug-to-Antibody Ratio (DAR) in the Synthesis of Antibody–Drug Conjugates (ADCs)

Lorenzo Angiolini, Fabrizio Manetti, Ottavia Spiga, Andrea Tafi, Anna Visibelli and Elena Petricci

J. Chem. Inf. Model., 2025, 65, 5847
DOI: 10.1021/acs.jcim.5c00037

Lysosomal-Cleavable Peptide Linkers in Antibody–Drug Conjugates

Seetharamsing Balamkundu and Chuan-Fa Liu

Biomedicines, 2023, 11, 3080
DOI: 10.3390/biomedicines11113080

Antibody-oligonucleotide conjugates for spatial proteomics: principles, applications, and challenges

Yinghui Qiu, Chunlan Li, Peiying Ye, Haiyun Zhang, Yanxiu Liu, Weiyan Ma, Chen Lin and Rongqin Ke

ABBS, 2025
DOI: 10.3724/abbs.2025212

Antibody-Drug Conjugates: A promising breakthrough in cancer therapy

Swapnali Parit, Ajit Manchare, Amol D. Gholap, Prashant Mundhe, Navnath Hatvate, Satish Rojekar and Vandana Patravale

International Journal of Pharmaceutics, 2024, 659, 124211
DOI: 10.1016/j.ijpharm.2024.124211

Crossing the Blood–Brain Barrier with Molecularly Imprinted Polymeric Nanocarriers: An Emerging Frontier in Brain Disease Therapy

Ranjit De, Shuliang Shi and Kyong‐Tai Kim

Advanced Science, 2026, 13
DOI: 10.1002/advs.202517004

Exploring Experimental and In Silico Approaches for Antibody–Drug Conjugates in Oncology Therapies

Vitor Martins de Almeida, Milena Botelho Pereira Soares and Osvaldo Andrade Santos-Filho

Pharmaceuticals, 2025, 18, 1198
DOI: 10.3390/ph18081198

Factors influencing the choice of monoclonal antibodies for antibody–drug conjugates

Md. Mahbub Hasan, Mark Laws, Peiqin Jin and Khondaker Miraz Rahman

Drug Discovery Today, 2022, 27, 354
DOI: 10.1016/j.drudis.2021.09.015

Antibody–drug conjugate as targeted therapeutics against hepatocellular carcinoma: preclinical studies and clinical relevance

M. Murali, A. R. Kumar, B. Nair, K. Pavithran, A. R. Devan, G. K. Pradeep and L. R. Nath

Clin Transl Oncol, 2022, 24, 407
DOI: 10.1007/s12094-021-02707-5

Bis‐ethynylphosphonamidates as an Modular Conjugation Platform to Generate Multi‐Functional Protein‐ and Antibody‐Drug‐Conjugates

Marc‐André Kasper, Lukas Lassak, Annette M. Vogl, Isabelle Mai, Jonas Helma, Dominik Schumacher and Christian P. R. Hackenberger

Eur J Org Chem, 2022, 2022
DOI: 10.1002/ejoc.202101389

Single‐Step N‐Terminal Modification of Proteins via a Bio‐Inspired Copper(II)‐Mediated Aldol Reaction

Kengo Hanaya, Kaho Yamoto, Kazuaki Taguchi, Kazuaki Matsumoto, Shuhei Higashibayashi and Takeshi Sugai

Chemistry A European J, 2022, 28
DOI: 10.1002/chem.202201677

Strategic and Chemical Advances in Antibody–Drug Conjugates

Ibrahim A. Alradwan, Meshal K. Alnefaie, Nojoud AL Fayez, Alhassan H. Aodah, Majed A. Majrashi, Meshael Alturki, Mohannad M. Fallatah, Fahad A. Almughem, Essam A. Tawfik and Abdullah A. Alshehri

Pharmaceutics, 2025, 17, 1164
DOI: 10.3390/pharmaceutics17091164

Targeted protein degradation through site-specific antibody conjugation with mannose 6-phosphate glycan

Kaori Mukai, Robert Cost, Xin Sheen Zhang, Emily Condiff, Joanne Cotton, Xiaohua Liu, Ekaterina Boudanova, Björn Niebel, Peter Piepenhagen, Xinming Cai, Anna Park and Qun Zhou

mAbs, 2024, 16
DOI: 10.1080/19420862.2024.2415333

Targeting HER2 Expressing Tumors with a Potent Drug Conjugate Based on an Albumin Binding Domain-Derived Affinity Protein

Javad Garousi, Haozhong Ding, Emma von Witting, Tianqi Xu, Anzhelika Vorobyeva, Maryam Oroujeni, Anna Orlova, Sophia Hober, Torbjörn Gräslund and Vladimir Tolmachev

Pharmaceutics, 2021, 13, 1847
DOI: 10.3390/pharmaceutics13111847

Recent advances in antibody glycoengineering for the gain of functions

Zhi Liu, Xiangman Zou, Feng Tang and Wei Huang

Current Opinion in Chemical Biology, 2024, 78, 102420
DOI: 10.1016/j.cbpa.2023.102420

Discovery of a Serine‐Directed Chemical Reaction for Site‐Specific Protein Modification via Phage Display Screening

Yingjie Lei, Kai Zhao, Mengzhun Guo, Liang Guo, Jinfeng Chen, Mengjiao Li, Dandan Liu, Kai Chen, Jiahao Mei, Tian Li, Bing Yang, Jing Huang and Bobo Dang

Angew Chem Int Ed, 2025, 64
DOI: 10.1002/anie.202514412

Immobilization of biotinylated antibodies through streptavidin binding aptamer

D. Brambilla, L. Sola, F. Damin, A. Mussida and M. Chiari

Talanta, 2023, 265, 124847
DOI: 10.1016/j.talanta.2023.124847

Antibody–Antibiotic Conjugates: Mechanisms, Clinical Progress, and Next‐Generation Strategies Against Multidrug‐Resistant Bacterial Infections

Parvin Askari, Soudabeh Eshaghi, Leila Omidvar and Motahareh Mahi‐Birjand

MicrobiologyOpen, 2026, 15
DOI: 10.1002/mbo3.70234

Designing antibodies as therapeutics

Paul J. Carter and Arvind Rajpal

Cell, 2022, 185, 2789
DOI: 10.1016/j.cell.2022.05.029

Site-specific conjugated antibody-element tags for single-cell ICP-MS

Haowen Hu, Zhengxian Lv, Yixin Guo, Li Yi, Limin Yang, Xiaowen Yan and Qiuquan Wang

Talanta, 2026, 300, 129227
DOI: 10.1016/j.talanta.2025.129227

Anti-HER2, High-DAR Antibody Fragment–Drug Conjugates with a Glucuronide-Based MMAE Linker–Payload Demonstrate Superior Efficacy over IgG-Based ADCs

Ioanna Stamati, Gokhan Yahioglu, Soraya Diez-Posada, Anja Pomowski, Isabel Perez-Castro, Ashleigh Stewart, Laura Bouché, Antony Constantinou, Benjamin J. Stenton, Savvas Saouros, Bryan Edwards, Sam Ness and Mahendra P. Deonarain

Molecular Cancer Therapeutics, 2025, 24, 1295
DOI: 10.1158/1535-7163.MCT-24-1182

Directed Functionalization of Recombinant Spider Silk Nonwoven Membranes with Antibodies Using Non‐Canonical Amino Acids

Claudia Lacombe, Charlotte Leonhardt, Martin Humenik, Birgit Wiltschi and Thomas Scheibel

Advanced Materials, 2026, 38
DOI: 10.1002/adma.202519707

Modular Assembly of Heterotrifunctional Molecules Enabled by Iodosulfonylation of Allenes and Subsequent Amination

Xiaofeng Lin, Chuxiong Peng, Shijie Liu, Jianpin Xiang, Binyan Lin, Qichen Zhan, Peng Cao and Tao Cao

J. Med. Chem., 2024, 67, 21251
DOI: 10.1021/acs.jmedchem.4c02114

Evaluation of Two Chemoenzymatic Glycan Remodeling Approaches to Generate Site-Specific Antibody–Drug Conjugates

Qiang Yang, He Chen, Chong Ou, Zhihao Zheng, Xiao Zhang, Yunpeng Liu, Guanghui Zong and Lai-Xi Wang

Antibodies, 2023, 12, 71
DOI: 10.3390/antib12040071

AJICAP Second Generation: Improved Chemical Site-Specific Conjugation Technology for Antibody–Drug Conjugate Production

Tomohiro Fujii, Yutaka Matsuda, Takuya Seki, Natsuki Shikida, Yusuke Iwai, Yuri Ooba, Kazutoshi Takahashi, Muneki Isokawa, Sayaka Kawaguchi, Noriko Hatada, Tomohiro Watanabe, Rika Takasugi, Akira Nakayama, Kazutaka Shimbo, Brian A. Mendelsohn, Tatsuya Okuzumi and Kei Yamada

Bioconjugate Chem., 2023
DOI: 10.1021/acs.bioconjchem.3c00040

Dual-payload antibody–drug conjugates: Taking a dual shot

Junjie Tao, Yilin Gu, Wei Zhou and Yuxi Wang

European Journal of Medicinal Chemistry, 2025, 281, 116995
DOI: 10.1016/j.ejmech.2024.116995

Antibody drug conjugates as targeted cancer therapy: past development, present challenges and future opportunities

Ritwik Maiti, Bhumika Patel, Nrupesh Patel, Mehul Patel, Alkesh Patel and Nirav Dhanesha

Arch. Pharm. Res., 2023, 46, 361
DOI: 10.1007/s12272-023-01447-0

Skin-Integrated Soft Wearable XR Interfaces for Seamless and Realistic User Experience

Kyung Rok Pyun, Jung Jae Park, Jiyong Ahn, Yoon Seon Lee, Hongchan Kim, Jinsol Kim, Sangjin Yoon, Kyoung-Ho Ha, Deog-Gyu Seo, John A. Rogers and Seung Hwan Ko

Chem. Rev., 2025, 125, 11567
DOI: 10.1021/acs.chemrev.4c00966

One‐Step Maleimide‐Based Dual Functionalization of Protein N‐Termini

Kengo Hanaya, Kazuaki Taguchi, Yuki Wada and Masaki Kawano

Angewandte Chemie, 2025, 137
DOI: 10.1002/ange.202417134

Galactose Oxidase Enables Modular Assembly of Conjugates from Native Antibodies with High Drug‐to‐Antibody Ratios**

Antonio Angelastro, Alexey Barkhanskiy, Ashley P. Mattey, Edward G. Pallister, Reynard Spiess, William Goundry, Perdita Barran and Sabine L. Flitsch

ChemSusChem, 2022, 15
DOI: 10.1002/cssc.202102592

Recent Advances in Chemical Protein Modification via Cysteine

Changliu Wang, Yongli Zhao and Junfeng Zhao

Chinese Journal of Organic Chemistry, 2022, 42, 2774
DOI: 10.6023/cjoc202203008

Microfabrication of engineered Lactococcus lactis biocarriers with genetically programmed immunorecognition probes for sensitive lateral flow immunoassay of antibiotic in milk and lake water

Fuyuan Zhang, Jiajie Chen, Fangkun Zhao, Minxuan Liu, Kaige Peng, Yuanhao Pu, Yaxin Sang, Shuo Wang and Xianghong Wang

Biosensors and Bioelectronics, 2024, 252, 116139
DOI: 10.1016/j.bios.2024.116139

Discovery of a Serine‐Directed Chemical Reaction for Site‐Specific Protein Modification via Phage Display Screening

Yingjie Lei, Kai Zhao, Mengzhun Guo, Liang Guo, Jinfeng Chen, Mengjiao Li, Dandan Liu, Kai Chen, Jiahao Mei, Tian Li, Bing Yang, Jing Huang and Bobo Dang

Angewandte Chemie, 2025, 137
DOI: 10.1002/ange.202514412

Orthogonal Site-Specific Dual Bioconjugation of Aryl and Alkyl Thiols

Mark A. R. de Geus, Christian E. Stieger, Jan Vincent V. Arafiles, Jean-Romain P. J. Lotthé, Peter Schmieder, Kristin Kemnitz-Hassanin, Beate Kindt, Heinrich Leonhardt, Saskia Schmitt, Marcus Gerlach, Dominik Schumacher, Jonas Helma, Marc-André Kasper and Christian P. R. Hackenberger

J. Am. Chem. Soc., 2025, 147, 18888
DOI: 10.1021/jacs.5c02981

Antibody Glycoengineering and Homogeneous Antibody‐Drug Conjugate Preparation

Shino Manabe and Yoshiki Yamaguchi

The Chemical Record, 2021, 21, 3005
DOI: 10.1002/tcr.202100054

A Toolkit for Engineering Proteins in Living Cells: Peptide with a Tryptophan-Selective Ru-TAP Complex to Regioselectively Photolabel Specific Proteins

Tzu-Ho Chen, Kevin Garnir, Chong-Yan Chen, Cheng-Bang Jian, Hua-De Gao, Bill Cheng, Mei-Chun Tseng, Cécile Moucheron, Andrée Kirsch-De Mesmaeker and Hsien-Ming Lee

J. Am. Chem. Soc., 2022, 144, 18117
DOI: 10.1021/jacs.2c08342

Antibody Drug Conjugate Formation Using 2‐14C‐Iminothiolane: A Radiochemical Analysis of Sequential Lysine Conjugation, Uncloaking of a Phantom Drug‐to‐Antibody Ratio, and Stability of the ADC

Michael Wallace, Michael J. Smith, John Brailsford, Difei Qiu, Alban J. Allentoff, Annie Tam, Selin Aytar, Michael Hay, Sharon Gong and Samuel Bonacorsi

Labelled Comp Radiopharmac, 2025, 68
DOI: 10.1002/jlcr.70002

Dithiol Based on l-Cysteine and Cysteamine as a Disulfide-Reducing Agent

Francesca Bartoccini, Michele Retini, Rita Crinelli, Michele Menotta, Alessandra Fraternale and Giovanni Piersanti

J. Org. Chem., 2022, 87, 10073
DOI: 10.1021/acs.joc.2c01050

Linker Design for the Antibody Drug Conjugates: A Comprehensive Review

Yaxin Lei, Minglei Zheng, Peng Chen, Chen Seng Ng, Teck Peng Loh and Huitao Liu

ChemMedChem, 2025, 20
DOI: 10.1002/cmdc.202500262

Site-specific construction of triptolide-based antibody-drug conjugates

Ding Wei, Yurong Mao, Zili Xu, Jiakang Chen, Jiusheng Li, Biao Jiang and Hongli Chen

Bioorganic & Medicinal Chemistry, 2021, 51, 116497
DOI: 10.1016/j.bmc.2021.116497

Tag‐Free Enzymatic Modification for Antibody−Drug Conjugate Production

Shunsuke Yamazaki and Yutaka Matsuda

ChemistrySelect, 2022, 7
DOI: 10.1002/slct.202203753

DVD-IgG1 antibody–drug conjugates: Expanding the landscape of targeted cancer therapy

Alexander F. Kiefer, Andrew D. Steele, Christoph Rader and Ben Shen

Current Opinion in Chemical Biology, 2026, 92, 102653
DOI: 10.1016/j.cbpa.2026.102653

Targeting cancer with antibody-drug conjugates: Promises and challenges

Alexis Q. Dean, Shen Luo, Julianne D. Twomey and Baolin Zhang

mAbs, 2021, 13
DOI: 10.1080/19420862.2021.1951427

One‐Step Assembly of Homogeneous DAR4 ADCs via a Traceless Fc Ligand‐Directed Acylation Strategy

Yue Zeng, Yuyu Lin, Qi Sun, Jiaying Hang, Wei Shi, Wei Huang and Feng Tang

ChemMedChem, 2026, 21
DOI: 10.1002/cmdc.202501075

Structural and Functional Insights into Viral and Fungal Proteins Involved in Chronic Inflammation and Their Biologic Treatments

Mohamed Halawa, Alicia L. Gallo and Valerie J. Carabetta

Pharmaceutics, 2025, 17, 1466
DOI: 10.3390/pharmaceutics17111466

Use of a Cyclic α-Alkylidene-β-Diketone as a Cleavable Linker Strategy for Antibody-Drug Conjugates

Juliana T. W. Tong, Makhdoom Sarwar, Marzieh Ahangarpour, Paul A. Hume, Geoffrey M. Williams, Margaret A. Brimble and Iman Kavianinia

J. Am. Chem. Soc., 2024, 146, 23717
DOI: 10.1021/jacs.4c04567

Cysteine‐Cysteine Cross‐Conjugation of both Peptides and Proteins with a Bifunctional Hypervalent Iodine‐Electrophilic Reagent

Ilias Koutsopetras, Abhaya Kumar Mishra, Rania Benazza, Oscar Hernandez‐Alba, Sarah Cianférani, Guilhem Chaubet, Stefano Nicolai and Jérôme Waser

Chemistry A European J, 2023, 29
DOI: 10.1002/chem.202302689

Perspectives on Nuclear Magnetic Resonance Spectroscopy in Drug Discovery Research

Janet Caceres-Cortes, Bradley Falk, Luciano Mueller and T G Murali Dhar

J. Med. Chem., 2024, 67, 1701
DOI: 10.1021/acs.jmedchem.3c02389

Review and prospects of targeted therapies for Spleen tyrosine kinase (SYK)

Zhaozhao Wang, Shu Qu, Jiahao Yuan, Wen Tian, Jinglei Xu, Rui Tao, Shilong Sun, Tao Lu, Weifang Tang and Yong Zhu

Bioorganic & Medicinal Chemistry, 2023, 96, 117514
DOI: 10.1016/j.bmc.2023.117514

Late-Stage N-Alkenylative Modifications of Indolic Scaffolds with Propiolates: Toward Bisconjugation and Macrocyclization

Xiaoye Chen, Chi-Ming Au, Pengyuan Fang, Yunsheng Xue, Ken Cham-Fai Leung and Wai-Lun Chan

Org. Lett., 2025, 27, 5081
DOI: 10.1021/acs.orglett.5c01162

Development and Recent Advances in Lysine and N-Terminal Bioconjugation for Peptides and Proteins

Ajcharapan Tantipanjaporn and Man-Kin Wong

Molecules, 2023, 28, 1083
DOI: 10.3390/molecules28031083

Chemical evolution of antibody–drug conjugates focused on linker design and conjugation strategies in hematology

Seungbin Park, Geetanjali B. Gone, Dohee Ahn and Sang J. Chung

Seminars in Hematology, 2025, 62, 289
DOI: 10.1053/j.seminhematol.2025.11.004

A Traceless Site‐Specific Conjugation on Native Antibodies Enables Efficient One‐Step Payload Assembly

Yue Zeng, Wei Shi, Qian Dong, Wanzhen Li, Jianxin Zhang, Xuelian Ren, Caihong Tang, Bo Liu, Yuanli Song, Yali Wu, Xingxing Diao, Hu Zhou, He Huang, Feng Tang and Wei Huang

Angewandte Chemie, 2022, 134
DOI: 10.1002/ange.202204132

Site-selective modification of native proteins

Yujun Kim, Han Bin Yi, Kyungdeok Seo, Hyun Soo Lee and Injae Shin

Trends in Chemistry, 2025, 7, 240
DOI: 10.1016/j.trechm.2025.03.003

Safety, dosimetry, and efficacy of an optimized long-acting somatostatin analog for peptide receptor radionuclide therapy in metastatic neuroendocrine tumors: From preclinical testing to first-in-human study

Wei Guo, Xuejun Wen, Yuhang Chen, Tianzhi Zhao, Jia Liu, Yucen Tao, Hao Fu, Hongjian Wang, Weizhi Xu, Yizhen Pang, Liang Zhao, Jingxiong Huang, Pengfei Xu, Zhide Guo, Weibing Miao, Jingjing Zhang, Xiaoyuan Chen and Haojun Chen

Acta Pharmaceutica Sinica B, 2025, 15, 707
DOI: 10.1016/j.apsb.2024.05.022

Expanding the potential of antibody–drug conjugates in gastrointestinal malignancies: beyond HER2 targets

P. Ntellas, A. Athauda, K. Sugiyama, M.L. Le, V. Crespi and I. Chau

ESMO Gastrointestinal Oncology, 2025, 8, 100154
DOI: 10.1016/j.esmogo.2025.100154

Single-Domain Antibodies as Antibody–Drug Conjugates: From Promise to Practice—A Systematic Review

Víctor Manuel Medina Pérez, Marta Baselga and Alberto J. Schuhmacher

Cancers, 2024, 16, 2681
DOI: 10.3390/cancers16152681

Hiding Payload Inside the IgG Fc Cavity Significantly Enhances the Therapeutic Index of Antibody–Drug Conjugates

Wei Shi, Jianxin Zhang, Liya Liu, Wanzhen Li, Zhi Liu, Anni Ren, Jie Wang, Caihong Tang, Yang Yang, Dandan Xu, Qianqian Huang, Yongqin Wang, Caili Luo, Wei Huang and Feng Tang

J. Med. Chem., 2023, 66, 1011
DOI: 10.1021/acs.jmedchem.2c01812

Therapeutic potential of antibody-drug conjugates possessing bifunctional anti-inflammatory action in the pathogenesis of rheumatoid arthritis

Tanu Dixit, Anuradha Vaidya and Selvan Ravindran

Arthritis Res Ther, 2024, 26
DOI: 10.1186/s13075-024-03452-0

Precision engineering of antibodies: A review of modification and design in the Fab region

Sa Wang, Yao Li, Jianfeng Mei, Shujiang Wu, Guoqing Ying and Yu Yi

International Journal of Biological Macromolecules, 2024, 275, 133730
DOI: 10.1016/j.ijbiomac.2024.133730

Ungesättigte Phosphinoxide für modulares Antikörper‐Rebridging und Einkomponenten Peptid‐Zyklisierung‐Biokonjugation

Christian E. Stieger, Alastair J. McMillan, Mark A. R. de Geus, Jan Vincent V. Arafiles, Luise Franz and Christian P. R. Hackenberger

Angewandte Chemie, 2025, 137
DOI: 10.1002/ange.202508656

Antibody–Drug Conjugates—Evolution and Perspectives

Adriana Aurelia Chis, Carmen Maximiliana Dobrea, Anca Maria Arseniu, Adina Frum, Luca-Liviu Rus, Gabriela Cormos, Cecilia Georgescu, Claudiu Morgovan, Anca Butuca, Felicia Gabriela Gligor and Andreea Loredana Vonica-Tincu

IJMS, 2024, 25, 6969
DOI: 10.3390/ijms25136969

Structure–Activity Relationships of Antibody-Drug Conjugates: A Systematic Review of Chemistry on the Trastuzumab Scaffold

Siddharth S. Matikonda, Ryan McLaughlin, Pradeep Shrestha, Carol Lipshultz and Martin J. Schnermann

Bioconjugate Chem., 2022, 33, 1241
DOI: 10.1021/acs.bioconjchem.2c00177

Overcoming Barriers in Cancer Biology Research: Current Limitations and Solutions

Giovanni Colonna

Cancers, 2025, 17, 2102
DOI: 10.3390/cancers17132102

Comparison of HER2-targeted affibody conjugates loaded with auristatin- and maytansine-derived drugs

Wen Yin, Tianqi Xu, Haozhong Ding, Jie Zhang, Vitalina Bodenko, Maria S. Tretyakova, Mikhail V. Belousov, Yongsheng Liu, Maryam Oroujeni, Anna Orlova, Vladimir Tolmachev, Torbjörn Gräslund and Anzhelika Vorobyeva

Journal of Controlled Release, 2023, 355, 515
DOI: 10.1016/j.jconrel.2023.02.005

Engineered Antibodies as Cancer Radiotheranostics

Zhenni Wei, Bingyu Li, Xuejun Wen, Vivianne Jakobsson, Peifei Liu, Xiaoyuan Chen and Jingjing Zhang

Advanced Science, 2024, 11
DOI: 10.1002/advs.202402361

Site-specific Antibody-Nitric Oxide Conjugate HN02 Possesses Improved Antineoplastic and Safety Properties

Tianyue Cheng, Jiajun Xie, Xun Yuan, Minji Guo, Jianbing Wu, Min Wang, Zhangjian Huang and Juan Zhang

Journal of Immunotherapy, 2024, 47, 149
DOI: 10.1097/CJI.0000000000000507