Stapling strategy enables improvement of antitumor activity and proteolytic stability of host-defense peptide hymenochirin-1B

Yulei Li, Minghao Wu, Qi Chang and Xia Zhao

RSC Adv., 2018, 8, 22268
DOI: 10.1039/C8RA03446J

Rational design of stapled peptides targeting phosphorylated GSK3β for regulating osteoclast differentiation

Tairong Liu, Wei Cong, Lei Ye, Xike Xu, Xiufei Liao, Gang Xie, Zhaoxi Cheng, Honggang Hu, Xiang Li and Hongli Liao

RSC Adv., 2020, 10, 7758
DOI: 10.1039/D0RA00008F

Non-reducible disulfide bond replacement implies that disulfide exchange is not required for hepcidin–ferroportin interaction

Dong-Liang Huang, Jing-Si Bai, Meng Wu, Xia Wang, Bernd Riedl, Elisabeth Pook, Carsten Alt, Marion Erny, Yi-Ming Li, Donald Bierer, Jing Shi and Ge-Min Fang

Chem. Commun., 2019, 55, 2821
DOI: 10.1039/C9CC00328B

Glucuronic acid as a helix-inducing linker in short peptides

Chongyang Wu, Huy N. Hoang, Ligong Liu and David P. Fairlie

Chem. Commun., 2018, 54, 2162
DOI: 10.1039/C7CC09785A

Chemical synthesis and biological activity of peptides incorporating an ether bridge as a surrogate for a disulfide bond

Rui Zhao, Pan Shi, Junyou Chen, Shuaishuai Sun, Jingnan Chen, Jibin Cui, Fangming Wu, Gemin Fang, Changlin Tian, Jing Shi, Donald Bierer, Lei Liu and Yi-Ming Li

Chem. Sci., 2020, 11, 7927
DOI: 10.1039/D0SC02374D

Synthesis of disulfide surrogate peptides incorporating an ethylene glycol bridge

Xiao-Xiong Wei, Ji-Bin Cui, Rui Zhao, Jie Luo, Yi-Ming Li, Donald Bierer and Jing Shi

New J. Chem., 2023, 47, 4213
DOI: 10.1039/D2NJ05290C

Chemical synthesis of disulfide surrogate peptides by using beta-carbon dimethyl modified diaminodiacids

Ji-Bin Cui, Xiao-Xiong Wei, Rui Zhao, Huixia Zhu, Jing Shi, Donald Bierer and Yi-Ming Li

Org. Biomol. Chem., 2021, 19, 9021
DOI: 10.1039/D1OB01715B

Cyclobutane-bearing restricted anchoring residues enabled geometry-specific hydrocarbon peptide stapling

Baobao Chen, Chao Liu, Wei Cong, Fei Gao, Yan Zou, Li Su, Lei Liu, Alexander Hillisch, Lutz Lehmann, Donald Bierer, Xiang Li and Hong-Gang Hu

Chem. Sci., 2023, 14, 11499
DOI: 10.1039/D3SC04279K

Dithiocarbamate-inspired side chain stapling chemistry for peptide drug design

Xiang Li, W. David Tolbert, Hong-Gang Hu, Neelakshi Gohain, Yan Zou, Fan Niu, Wang-Xiao He, Weirong Yuan, Jia-Can Su, Marzena Pazgier and Wuyuan Lu

Chem. Sci., 2019, 10, 1522
DOI: 10.1039/C8SC03275K

Cytotoxic and antitumor peptides as novel chemotherapeutics

Xin Luan, Ye Wu, Yi-Wen Shen, Hong Zhang, Yu-Dong Zhou, Hong-Zhuan Chen, Dale G. Nagle and Wei-Dong Zhang

Nat. Prod. Rep., 2021, 38, 7
DOI: 10.1039/D0NP00019A

Modulating Secondary Structure Motifs Through Photo‐Labile Peptide Staples

Ilze Lāce, Sophia Bazzi, Jon Uranga, Anastasiya Schirmacher, Ulf Diederichsen, Ricardo A. Mata and Nadja A. Simeth

ChemBioChem, 2023, 24
DOI: 10.1002/cbic.202300270

Different stapling-based peptide drug design: Mimicking α-helix as inhibitors of protein–protein interaction

Xiang Li, Yan Zou and Hong-Gang Hu

Chinese Chemical Letters, 2018, 29, 1088
DOI: 10.1016/j.cclet.2018.01.018

Systematical Mutational Analysis of FRATtide against Osteoclast Differentiation by Alanine Scanning

Yi Yang, Chenchen Geng, Huaxing Shen, Jingru Chao, Zhe Wang, Wei Cong, Xiang Li, Guangming Ye and Yunyun Jiang

ACS Med. Chem. Lett., 2024, 15, 1242
DOI: 10.1021/acsmedchemlett.4c00127

Advances in Hydrocarbon Stapled Peptides via Ring‐Closing Metathesis: Synthetic Strategies, Structural Diversity, and Therapeutic Applications

Linji Li, Rong Li, Yanan Jiang, Jingru Chao, Si Chen, Hongli Liao and Xiang Li

ChemBioChem, 2025, 26
DOI: 10.1002/cbic.202500527

Design, Synthesis and Antifungal Activity of Stapled Aurein1.2 Peptides

Mengjun Zheng, Ruina Wang, Si Chen, Yan Zou, Lan Yan, Linjing Zhao and Xiang Li

Antibiotics, 2021, 10, 956
DOI: 10.3390/antibiotics10080956

Methodology of stable peptide based on propargylated sulfonium

Heng Li, Zhanfeng Hou, Yuena Wang, Ziyuan Zhou, Jin Cai, Qilei Xin, Feng Yin, Zigang Li and Naihan Xu

Biochemistry and Biophysics Reports, 2023, 35, 101508
DOI: 10.1016/j.bbrep.2023.101508

Discovery of an orally effective double-stapled peptide for reducing ovariectomy-induced bone loss in mice

Wei Cong, Huaxing Shen, Xiufei Liao, Mengjun Zheng, Xianglong Kong, Zhe Wang, Si Chen, Yulei Li, Honggang Hu and Xiang Li

Acta Pharmaceutica Sinica B, 2023, 13, 3770
DOI: 10.1016/j.apsb.2023.05.004

Hydrocarbon stapling modification of peptide alyteserin‐2a: Discovery of novel stapled peptide antitumor agents

Ziqiang Yu, Hua Tang, Wei Cong, Fei Gao, Huaqiang Li, Honggang Hu, Xiaoyan Wang and Shipeng He

Journal of Peptide Science, 2022, 28
DOI: 10.1002/psc.3401

Chemical synthesis and structural analysis of guanylate cyclase C agonist linaclotide

Chenchen Chen, Shuai Gao, Qian Qu, Pengcheng Mi, Anjin Tao and Yi-Ming Li

Chinese Chemical Letters, 2018, 29, 1135
DOI: 10.1016/j.cclet.2018.01.005

Discovery, structure, and chemical synthesis of disulfide-rich peptide toxins and their analogs

Ge-Min Fang, Xiao-Xu Chen, Qian-Qian Yang, Liang-Jing Zhu, Ning-Ning Li, Hai-Zhu Yu and Xiang-Ming Meng

Chinese Chemical Letters, 2018, 29, 1033
DOI: 10.1016/j.cclet.2018.02.002

Effects of Glycosylation and d-Amino Acid Substitution on the Antitumor and Antibacterial Activities of Bee Venom Peptide HYL

Ming-hao Wu, Su Ai, Qing Chen, Xiang-yan Chen, Hong-jin Li, Yu-lei Li and Xia Zhao

Bioconjugate Chem., 2020, 31, 2293
DOI: 10.1021/acs.bioconjchem.0c00355

Design, synthesis, and anti-tumor activities of novel Brevinin-1BYa peptidomimetics

Shili Xiong, Nan Wang, Chao Liu, Huaxing Shen, Zengqiang Qu, Lijun Zhu, Xiaosong Bai, Hong-gang Hu, Wei Cong and Liang Zhao

Bioorganic & Medicinal Chemistry Letters, 2021, 37, 127831
DOI: 10.1016/j.bmcl.2021.127831

Macrocyclic α helical peptide therapeutic modality: A perspective of learnings and challenges

Tomi K. Sawyer, Anthony W. Partridge, Hung Yi Kristal Kaan, Yu-Chi Juang, Shuhui Lim, Charles Johannes, Tsz Ying Yuen, Chandra Verma, Srinivasaraghavan Kannan, Pietro Aronica, Yaw Sing Tan, Brad Sherborne, Sookhee Ha, Jerome Hochman, Shiying Chen, Laura Surdi, Andrea Peier, Berengere Sauvagnat, Peter J. Dandliker, Christopher J. Brown, Simon Ng, Fernando Ferrer and David P. Lane

Bioorganic & Medicinal Chemistry, 2018, 26, 2807
DOI: 10.1016/j.bmc.2018.03.008

Recent structural advances in constrained helical peptides

Kornelia J. Skowron, Thomas E. Speltz and Terry W. Moore

Medicinal Research Reviews, 2019, 39, 749
DOI: 10.1002/med.21540

The Impact of Adrenomedullin Thr22 on Selectivity within the Calcitonin Receptor‐like Receptor/Receptor Activity‐Modifying Protein System

Jan‐Patrick Fischer, Sylvia Els‐Heindl, Ria Schönauer, Donald Bierer, Johannes Köbberling, Bernd Riedl and Annette G. Beck‐Sickinger

ChemMedChem, 2018, 13, 1797
DOI: 10.1002/cmdc.201800329

Facilitating the structural characterisation of non-canonical amino acids in biomolecular NMR

Sarah Kuschert, Martin Stroet, Yanni Ka-Yan Chin, Anne Claire Conibear, Xinying Jia, Thomas Lee, Christian Reinhard Otto Bartling, Kristian Strømgaard, Peter Güntert, Karl Johan Rosengren, Alan Edward Mark and Mehdi Mobli

Magn. Reson., 2023, 4, 57
DOI: 10.5194/mr-4-57-2023

Total synthesis of TRADD death domain with arginine N-GlcNAcylation by hydrazide-based native chemical ligation

Ye Wu, Yulei Li, Wei Cong, Yan Zou, Xiang Li and Honggang Hu

Chinese Chemical Letters, 2020, 31, 107
DOI: 10.1016/j.cclet.2019.05.010

Development of a penetratin-conjugated stapled peptide that inhibits Wnt/β-catenin signaling

Keisuke Tsuchiya, Masato Kiyoshi, Noritaka Hashii, Minami Fujita, Takashi Kurohara, Akiko Ishii-Watabe, Kiyoshi Fukuhara, Takashi Misawa and Yosuke Demizu

Bioorganic & Medicinal Chemistry, 2022, 73, 117021
DOI: 10.1016/j.bmc.2022.117021

Advances in the Study of Structural Modification and Biological Activities of Anoplin

Ye Wu, Rui Huang, Jin-Mei Jin, Li-Jun Zhang, Hong Zhang, Hong-Zhuan Chen, Li-Li Chen and Xin Luan

Front. Chem., 2020, 8
DOI: 10.3389/fchem.2020.00519

Stapled Wasp Venom-Derived Oncolytic Peptides with Side Chains Induce Rapid Membrane Lysis and Prolonged Immune Responses in Melanoma

Ye Wu, Dong Lu, Yixin Jiang, Jinmei Jin, Sanhong Liu, Lili Chen, Hong Zhang, Yudong Zhou, Hongzhuan Chen, Dale G. Nagle, Xin Luan and Weidong Zhang

J. Med. Chem., 2021, 64, 5802
DOI: 10.1021/acs.jmedchem.0c02237

Synthesis of Quaternary α-Fluorinated α-Amino Acid Derivatives via Coordinating Cu(II) Catalytic α-C(sp3)–H Direct Fluorination

Qiang Wei, Yao Ma, Li Li, Qingfei Liu, Zijie Liu and Gang Liu

Org. Lett., 2018, 20, 7100
DOI: 10.1021/acs.orglett.8b03044

Peptide stapling with the retention of double native side-chains

Ye Wu, Yan Zou, Lingling Sun, Alfredo Garzino-Demo, Honggang Hu, Weidong Zhang and Xiang Li

Chinese Chemical Letters, 2021, 32, 4045
DOI: 10.1016/j.cclet.2021.04.030

Discovery of a novel antifungal agent: All‐hydrocarbon stapling modification of peptide Aurein1.2

Mengjun Zheng, Huixuan Chen, Xiang Li, Si Chen, Yejiao Shi and Honggang Hu

Journal of Peptide Science, 2024, 30
DOI: 10.1002/psc.3533

Structural Modification and Antitumor Activity Study of Peptide Codesane: Discovery of Novel Stapled Peptide Antitumor Agents

Qingmei Li, Lijuan Qiu and Yong Li

Journal of Peptide Science, 2025, 31
DOI: 10.1002/psc.70012

Improving Selectivity, Proteolytic Stability, and Antitumor Activity of Hymenochirin-1B: A Novel Glycosylated Staple Strategy

Yulei Li, Yihan Zhang, Minghao Wu, Qi Chang, Honggang Hu and Xia Zhao

ACS Chem. Biol., 2019, 14, 516
DOI: 10.1021/acschembio.9b00046

Recognition of ASF1 by Using Hydrocarbon‐Constrained Peptides

May Bakail, Silvia Rodriguez‐Marin, Zsófia Hegedüs, Marie E. Perrin, Françoise Ochsenbein and Andrew J. Wilson

ChemBioChem, 2019, 20, 891
DOI: 10.1002/cbic.201800633

Structure-based development of an osteoprotegerin-like glycopeptide that blocks RANKL/RANK interactions and reduces ovariectomy-induced bone loss in mice

Chao Liu, Xiao Chen, Xin Zhi, Weizong Weng, Quan Li, Xiang Li, Yan Zou, Jiacan Su and Hong-Gang Hu

European Journal of Medicinal Chemistry, 2018, 145, 661
DOI: 10.1016/j.ejmech.2018.01.022

Cysteine [2,4] Disulfide Bond as a New Modifiable Site of α-Conotoxin TxIB

Baojian Zhang, Maomao Ren, Yang Xiong, Haonan Li, Yong Wu, Ying Fu, Dongting Zhangsun, Shuai Dong and Sulan Luo

Marine Drugs, 2021, 19, 119
DOI: 10.3390/md19020119

Facile Asymmetric Synthesis of α,α-Disubstituted Amino Acid Derivatives with Gold Redox Catalysis Using a Chiral Auxiliary

Teng Yuan, Qi Tang, Kelton Radefeld, Xiaohan Ye, Chuan Shan, Kai Zhao, Jaclyn Bredenkamp, Peter Y. Zavalij and Xiaodong Shi

ACS Catal., 2025, 15, 14845
DOI: 10.1021/acscatal.5c02965

Structural modification and antitumor activity of antimicrobial peptide HYL

Minghao Wu, Qing Chen, Yingdi Wang, Yulei Li, Xia Zhao and Qi Chang

Chinese Chemical Letters, 2020, 31, 1288
DOI: 10.1016/j.cclet.2019.10.013

Stapled Helical Peptides Bearing Different Anchoring Residues

Xiang Li, Si Chen, Wei-Dong Zhang and Hong-Gang Hu

Chem. Rev., 2020, 120, 10079
DOI: 10.1021/acs.chemrev.0c00532

Macrocyclic Control in Helix Mimetics

Danielle A. Guarracino, Jacob A. Riordan, Gianna M. Barreto, Alexis L. Oldfield, Christopher M. Kouba and Desiree Agrinsoni

Chem. Rev., 2019, 119, 9915
DOI: 10.1021/acs.chemrev.8b00623

Design, synthesis, and biological evaluation of stapled ascaphin-8 peptides

Jing Liu, Si Chen, Xiao-Yun Chai, Fei Gao, Chen Wang, Hua Tang, Xiang Li, Ying Liu and Hong-Gang Hu

Bioorganic & Medicinal Chemistry, 2021, 40, 116158
DOI: 10.1016/j.bmc.2021.116158

Design and synthesis of Nrf2-derived hydrocarbon stapled peptides for the disruption of protein-DNA-interactions

Bianca Wiedemann, Dominic Kamps, Laura Depta, Jörn Weisner, Jana Cvetreznik, Stefano Tomassi, Sascha Gentz, Jan-Erik Hoffmann, Matthias P. Müller, Oliver Koch, Leif Dehmelt, Daniel Rauh and Alessio Lodola

PLoS ONE, 2022, 17, e0267651
DOI: 10.1371/journal.pone.0267651

Recent advances in chemical protein synthesis: method developments and biological applications

Suwei Dong, Ji-Shen Zheng, Yiming Li, Huan Wang, Gong Chen, Yongxiang Chen, Gemin Fang, Jun Guo, Chunmao He, Honggang Hu, Xuechen Li, Yanmei Li, Zigang Li, Man Pan, Shan Tang, Changlin Tian, Ping Wang, Bian Wu, Chuanliu Wu, Junfeng Zhao and Lei Liu

Sci. China Chem., 2024, 67, 1060
DOI: 10.1007/s11426-024-1950-1

Interchain doubly-bridged α-helical peptides for the development of protein binders

Yaqi Chen, Jingjing Liang, Tao Li, Ping Lin, Yibing Zhao and Chuanliu Wu

Chinese Chemical Letters, 2019, 30, 924
DOI: 10.1016/j.cclet.2019.02.013