Institute of Chemical Sciences and Engineering, School of Basic Sciences, École Polytechnique Fédérale de Lausanne (EPFL), CH-1015, Lausanne, Switzerland.
Angew Chem Int Ed Engl. 2024 Jan 15;63(3):e202308251. doi: 10.1002/anie.202308251. Epub 2023 Oct 23.
Cyclic peptides are fascinating molecules abundantly found in nature and exploited as molecular format for drug development as well as other applications, ranging from research tools to food additives. Advances in peptide technologies made over many years through improved methods for synthesis and drug development have resulted in a steady stream of new drugs, with an average of around one cyclic peptide drug approved per year. Powerful technologies for screening random peptide libraries, and de novo generating ligands, have enabled the development of cyclic peptide drugs independent of naturally derived molecules and now offer virtually unlimited development opportunities. In this review, we feature therapeutically relevant cyclic peptides derived from nature and discuss the unique properties of cyclic peptides, the enormous technological advances in peptide ligand development in recent years, and current challenges and opportunities for developing cyclic peptides that address unmet medical needs.
环肽是自然界中大量存在的一种引人入胜的分子，被广泛用作药物开发以及其他应用的分子形式，从研究工具到食品添加剂。多年来，通过改进的合成和药物开发方法，肽技术取得了进展，导致了新药物的不断涌现，平均每年约有一种环肽药物获得批准。用于筛选随机肽文库和从头生成配体的强大技术，使得独立于天然衍生分子开发环肽药物成为可能，现在提供了几乎无限的发展机会。在这篇综述中，我们介绍了来自自然界的具有治疗意义的环肽，并讨论了环肽的独特性质、近年来肽配体开发方面的巨大技术进步，以及开发解决未满足医疗需求的环肽所面临的挑战和机遇。
