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光诱导自由基硫醇-烯反应:基于肽的药物设计的多功能工具包。

Photo-induced radical thiol-ene chemistry: a versatile toolbox for peptide-based drug design.

机构信息

School of Chemical Sciences, The University of Auckland, 23 Symonds Street, Auckland 1010, New Zealand.

出版信息

Chem Soc Rev. 2021 Jan 21;50(2):898-944. doi: 10.1039/d0cs00354a. Epub 2021 Jan 6.

DOI:10.1039/d0cs00354a
PMID:33404559
Abstract

While the global market for peptide/protein-based therapeutics is witnessing significant growth, the development of peptide drugs remains challenging due to their low oral bioavailability, poor membrane permeability, and reduced metabolic stability. However, a toolbox of chemical approaches has been explored for peptide modification to overcome these obstacles. In recent years, there has been a revival of interest in photoinduced radical thiol-ene chemistry as a powerful tool for the construction of therapeutic peptides.

摘要

尽管基于肽/蛋白质的治疗药物的全球市场正在见证显著的增长,但由于肽类药物的口服生物利用度低、膜通透性差和代谢稳定性降低,其开发仍然具有挑战性。然而,已经探索了一系列化学方法来修饰肽以克服这些障碍。近年来,光诱导自由基硫醇-烯反应作为构建治疗性肽的有力工具重新引起了人们的兴趣。

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