Zorzi Alessandro, Deyle Kaycie, Heinis Christian
Institute of Chemical Sciences and Engineering, Ecole Polytechnique Fédérale de Lausanne (EPFL), CH-1015 Lausanne, Switzerland.
Institute of Chemical Sciences and Engineering, Ecole Polytechnique Fédérale de Lausanne (EPFL), CH-1015 Lausanne, Switzerland.
Curr Opin Chem Biol. 2017 Jun;38:24-29. doi: 10.1016/j.cbpa.2017.02.006. Epub 2017 Feb 27.
Cyclic peptides combine several favorable properties such as good binding affinity, target selectivity and low toxicity that make them an attractive modality for the development of therapeutics. Over 40 cyclic peptide drugs are currently in clinical use and around one new cyclic peptide drug enters the market every year on average. The vast majority of clinically approved cyclic peptides are derived from natural products, such as antimicrobials or human peptide hormones. New powerful techniques based on rational design and in vitro evolution have enabled the de novo development of cyclic peptide ligands to targets for which nature does not offer solutions. A look at the cyclic peptides currently under clinical evaluation shows that several have been developed using such techniques. This new source for cyclic peptide ligands introduces a freshness to the field, and it is likely that de novo developed cyclic peptides will be in clinical use in the near future.
环肽具有多种有利特性，如良好的结合亲和力、靶标选择性和低毒性，这些特性使其成为极具吸引力的治疗药物开发形式。目前有40多种环肽药物正在临床使用，平均每年约有一种新的环肽药物进入市场。绝大多数临床批准的环肽都源自天然产物，如抗菌剂或人类肽激素。基于合理设计和体外进化的新强大技术，使得能够从头开发针对自然界未提供解决方案的靶标的环肽配体。看看目前正在临床评估的环肽就会发现，其中几种就是使用此类技术开发的。这种环肽配体的新来源为该领域带来了新气象，从头开发的环肽很可能在不久的将来投入临床使用。
