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Current development of bicyclic peptides

Feng, Dazhi; Liu, Lihua; Shi, Yuqi; Du, Pian; Xu, Shengtao; Zhu, Zheying; Xu, Jinyi; Yao, Hong


Dazhi Feng

Lihua Liu

Yuqi Shi

Pian Du

Shengtao Xu

Associate Professor in International Pharmacy and Traditional Medicines

Jinyi Xu

Hong Yao


Bicyclic peptides, a class of polypeptides with two loops within their structure, have emerged as powerful tools in the development of new peptide drugs. They have the potential to bind to challenged drug targets, with antibody-like affinity and selectivity. Meanwhile, bicyclic peptides possess small molecule-like access to chemical synthesis, which is conducive to large-scale synthesis and screening. In the last five years, bicyclic peptide technology has been increasingly developed, and researchers have carried out a variety of studies to elucidate the potential functions of bicyclic peptides. With the continuous development of synthetic methods and the advances of new technology to build bicyclic peptide libraries, bicyclic peptides are now becoming widely used in the development of new drugs for various diseases. This perspective provides an overview of the structure types, synthesis and applications of bicyclic peptides in current drug development, and our own views on future challenges of bicyclic peptides.


Feng, D., Liu, L., Shi, Y., Du, P., Xu, S., Zhu, Z., …Yao, H. (2023). Current development of bicyclic peptides. Chinese Chemical Letters, 34(6), Article 108026.

Journal Article Type Article
Acceptance Date Nov 28, 2022
Online Publication Date Nov 29, 2022
Publication Date 2023-06
Deposit Date Dec 2, 2022
Publicly Available Date Nov 30, 2023
Journal Chinese Chemical Letters
Print ISSN 1001-8417
Publisher Elsevier BV
Peer Reviewed Peer Reviewed
Volume 34
Issue 6
Article Number 108026
Keywords General Chemistry
Public URL
Publisher URL


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