Development of sulfonyl fluoride chemical probes to advance the discovery of cereblon modulators

Yingpeng Liu, Radosław P. Nowak, Jianwei Che, Katherine A. Donovan, Fidel Huerta, Hu Liu, Rebecca J. Metivier, Eric S. Fischer and Lyn H. Jones

RSC Med. Chem., 2024, 15, 607
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Development of a covalent cereblon-based PROTAC employing a fluorosulfate warhead

Radosław P. Nowak, Leah Ragosta, Fidel Huerta, Hu Liu, Scott B. Ficarro, Justin T. Cruite, Rebecca J. Metivier, Katherine A. Donovan, Jarrod A. Marto, Eric S. Fischer, Breanna L. Zerfas and Lyn H. Jones

RSC Chem. Biol., 2023, 4, 906
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Which Small Molecule? Selecting Chemical Probes for Use in Cancer Research and Target Validation

Mary M. Mader, Joachim Rudolph, Ingo V. Hartung, David Uehling, Paul Workman and William Zuercher

Cancer Discovery, 2023, 13, 2150
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Research Progress in Targeting GSPT1: Molecular Glues, Bifunctional Degraders, and Antibody-Enabled Molecular Glues for Cancer Therapy

Binbin Cheng, Yaping Wang, Yimeng Hong, Yingxing Zhou, Jianjun Chen and Chunlai Zeng

J. Med. Chem., 2025, 68, 13169
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C2H2 Zinc Finger Transcription Factors Associated with Hemoglobinopathies

Xing Zhang, Fangfang Xia, Xiaotian Zhang, Robert M. Blumenthal and Xiaodong Cheng

Journal of Molecular Biology, 2024, 436, 168343
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Targeted Protein Degradation: Mechanisms, Therapeutic Applications, Challenges, and Future Directions

Poovarasan B. and Sivakumar G.

International Journal of Innovative Science and Research Technology (IJISRT), 2025, 1744
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Optimization and Evaluation of Complementary Degrader Discovery Assays for Application in Screening

Johanna Huchting, Arjen Weller, Moyra Schweizer, Mona Brandt, Jan Heering, Maria Kuzikov, Markus Wolf, Jeanette Reinshagen, Markus A. Queisser, Philip Gribbon, Andrea Zaliani, Ole Pless and Aimo Kannt

ACS Pharmacol. Transl. Sci., 2025, 8, 2600
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Design and synthetic approaches to thalidomide based small molecule degraders

Ajeet Kumar, Gulshan Kumar, Nidhi Kalia and Priya Ranjan Sahoo

European Journal of Medicinal Chemistry, 2025, 293, 117700
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An engineered cereblon optimized for high-throughput screening and molecular glue discovery

Henry J. Bailey, Jonathan Eisert, Rubina Kazi, Jan Gerhartz, Dominika Ewa Pieńkowska, Ina Dressel, Joshua Vollrath, Ivan Kondratov, Tetiana Matviyuk, Nataliya Tolmachova, Varun Jayeshkumar Shah, Giulio Giuliani, Thorsten Mosler, Thomas M. Geiger, Ana M. Esteves, Sandra P. Santos, Raquel L. Sousa, Tiago M. Bandeiras, Eva-Maria Leibrock, Ulrike Bauer, Birgitta Leuthner, Julian D. Langer, Ansgar A. Wegener, Radosław P. Nowak, Fiona J. Sorrell and Ivan Dikic

Cell Chemical Biology, 2025, 32, 363
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From Thalidomide to Rational Molecular Glue Design for Targeted Protein Degradation

Vladas Oleinikovas, Pablo Gainza, Thomas Ryckmans, Bernhard Fasching and Nicolas H. Thomä

Annu. Rev. Pharmacol. Toxicol., 2024, 64, 291
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E3 ubiquitin ligase TRIM31: A potential therapeutic target

Nian-Hua Deng, Zhen Tian, Ying-Jiao Zou and Shou-Bo Quan

Biomedicine & Pharmacotherapy, 2024, 176, 116846
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Thalidomide-induced limb malformations: an update and reevaluation

Michael D. Collins and William J. Scott

Arch Toxicol, 2025, 99, 1643
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Asymmetric Dirhodium-Catalyzed Modification of Immunomodulatory Imide Drugs and Their Biological Assessment

William F. Tracy, Geraint H. M. Davies, Lei Jia, Ethan D. Evans, Zhenghang Sun, Jennifer Buenviaje, Gody Khambatta, Shan Yu, Lihong Shi, Veerabahu Shanmugasundaram, Jesus Moreno, Emily C. Cherney and Huw M. L. Davies

ACS Med. Chem. Lett., 2024, 15, 1575
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Monoselective Histone Deacetylase 6 PROTAC Degrader Shows In Vivo Tractability

Harsimran K. Garcha, Olasunkanmi O. Olaoye, Abootaleb Sedighi, Daniel Pölöske, Pearla Hariri, Wenlong Yu, Diaaeldin I. Abdallah, Richard Moriggl, Elvin D. de Araujo and Patrick T. Gunning

J. Med. Chem., 2025, 68, 6165
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The advancement of ubiquitination regulation in apoptosis, ferroptosis, autophagy, drug resistance and treatment of cancer

Hui Ling, Shuyao Xiao, Yalin Lei, Yujie Zhou, Jiaying Tan, Xiaojie Chen, Da Ma, Can Liang, Qingyi Liu, Wei Liu and Tiebing Zeng

Archives of Biochemistry and Biophysics, 2025, 771, 110497
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The changing landscape of medicinal chemistry optimization

Anita Rácz, Levente M. Mihalovits, Maximilian Beckers, Nikolas Fechner, Nikolaus Stiefl, Finton Sirockin, William McCoull, Emma Evertsson, Malin Lemurell, Gergely Makara and György M. Keserű

Nat Rev Drug Discov, 2025
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Single-Molecule-Based, Label-Free Monitoring of Molecular Glue Efficacies for Promoting Protein–Protein Interactions Using YaxAB Nanopores

Minju Ryu, Sohee Oh, Ki-Baek Jeong, Sungbo Hwang, Jin-Sik Kim, Minji Chung and Seung-Wook Chi

ACS Nano, 2024, 18, 31451
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Discovery of CRBN-Dependent WEE1 Molecular Glue Degraders from a Multicomponent Combinatorial Library

Hlib Razumkov, Zixuan Jiang, Kheewoong Baek, Inchul You, Qixiang Geng, Katherine A. Donovan, Michelle T. Tang, Rebecca J. Metivier, Nada Mageed, Pooreum Seo, Zhengnian Li, Woong Sub Byun, Stephen M. Hinshaw, Roman C. Sarott, Eric S. Fischer and Nathanael S. Gray

J. Am. Chem. Soc., 2024, 146, 31433
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Characterization of a dual degrader of MDM2 and GSPT1

Ira Tandon, Paulina N. Esguerra, Chunrong Li, Huan Sun, Ka Yang, Zhongrui Zhang, Junmin Peng and Weiping Tang

European Journal of Medicinal Chemistry, 2025, 295, 117793
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Screening for molecular glues – Challenges and opportunities

Geoffrey A. Holdgate, Catherine Bardelle, Sophia K. Berry, Alice Lanne and Maria Emanuela Cuomo

SLAS Discovery, 2024, 29, 100136
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Expanding the druggable zinc-finger proteome defines properties of drug-induced degradation

Mikołaj Słabicki, Jiho Park, Radosław P. Nowak, Shourya S. Roy Burman, Jesse Pellman, Charles Zou, Hlib Razumkov, Jeannie Carreiro, Simran Rastogi, Anna Goldstein, Marek M. Nagiec, Katherine A. Donovan, Jianwei Che, Moritz Hunkeler, Qixiang Geng, Chi-Lin Hsu, Megha Lakshminarayan, Chelsea Shu, Rebecca L. Zon, Zuzanna Kozicka, Paul M.C. Park, Jonathan M. Tsai, Hojong Yoon, Lyn H. Jones, Adam S. Sperling, Nathanael S. Gray, Eric S. Fischer and Benjamin L. Ebert

Molecular Cell, 2025, 85, 3184
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Targeted protein degradation in CNS disorders: a promising route to novel therapeutics?

Sandra Kuemper, Andrew G. Cairns, Kristian Birchall, Zhi Yao and Jonathan M. Large

Front. Mol. Neurosci., 2024, 17
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The “three body solution”: Structural insights into molecular glues

Aidan C.A. Tomlinson, John E. Knox, Luc Brunsveld, Christian Ottmann and Jason K. Yano

Current Opinion in Structural Biology, 2025, 91, 103007
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Application of Weighted Interaction-Fingerprints for Rationalizing Neosubstrate Potency and Selectivity of Cereblon-Based Molecular Glues

Guilian Luchini, Shuang Liu, Hannah L. Powers, Emily Cherney, Jinyi Zhu, Kristina Danga, Joel W. Thompson, Lihong Shi, Barbra Pagarigan, Dong Donna Wei, Peter Park, Andrew P. Degnan, Christoph W. Zapf, Jennifer R. Riggs, Scott Johnson and Thomas Cummins

J. Med. Chem., 2025, 68, 20657
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Discovery of novel benzosultam CRBN ligands

Hoyeong Park, Santosh Shivanand Raikar, Yonghyo Kim, Chong Hak Chae, Yong‐Hee Cho and Pilho Kim

Bulletin Korean Chem Soc, 2025, 46, 48
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Property-Based Optimization of Cereblon-Based Molecular Glue Degraders

Lyn H. Jones

ACS Med. Chem. Lett., 2025, 16, 1456
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High cereblon expression in neuroendocrine cancer confers vulnerability to GSPT1 molecular glue degrader

Jaewoo Park, Min Sung Joo, Myung Jun Kim, Seungseok Oh, Phuong Thao Tran, Minju Kwon, Yong June Choi, JaeYung Lee, Eun-Jung Kim, Dong Hyuk Ki, Hunmi Choi, Wooseok Han and Keon Wook Kang

Exp Hematol Oncol, 2025, 14
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