Gang Donghyeok, Kim Do Wook, Park Hee-Sung
Department of Chemistry, Korea Advanced Institute of Science and Technology, 291 Daehak-ro, Yuseong-gu, Daejeon 34141, Korea.
Genes (Basel). 2018 Nov 16;9(11):557. doi: 10.3390/genes9110557.
To date, small molecules and macromolecules, including antibodies, have been the most pursued substances in drug screening and development efforts. Despite numerous favorable features as a drug, these molecules still have limitations and are not complementary in many regards. Recently, peptide-based chemical structures that lie between these two categories in terms of both structural and functional properties have gained increasing attention as potential alternatives. In particular, peptides in a circular form provide a promising scaffold for the development of a novel drug class owing to their adjustable and expandable ability to bind a wide range of target molecules. In this review, we discuss recent progress in methodologies for peptide cyclization and screening and use of bioactive cyclic peptides in various applications.
迄今为止,小分子和大分子,包括抗体,一直是药物筛选和开发工作中最受关注的物质。尽管作为药物有许多有利特性,但这些分子仍有局限性,在许多方面并不互补。最近,在结构和功能特性方面介于这两类之间的基于肽的化学结构作为潜在的替代物受到了越来越多的关注。特别是,环状肽由于其能够结合广泛靶分子的可调节和可扩展能力,为新型药物类别的开发提供了一个有前景的支架。在这篇综述中,我们讨论了肽环化方法以及生物活性环肽在各种应用中的筛选和使用方面的最新进展。