Current development of bicyclic peptides

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. (c) 2023 Published by Elsevier B.V. on behalf of Chinese Chemical Society and Institute of Materia Medica, Chinese Academy of Medical Sciences.

Automated summary

Bicyclic peptides, with two loops within their structure, have emerged as powerful tools in the development of new peptide drugs due to their potential to bind to challenged drug targets with antibody-like affinity and selectivity. They also possess small molecule-like access to chemical synthesis, enabling large-scale synthesis and screening. This perspective provides an overview of the structure types, synthesis, and applications of bicyclic peptides in current drug development and discusses future challenges.