拟肽
环丙烷
化学
合理设计
生物分子
立体化学
组合化学
计算生物学
肽
生物化学
纳米技术
生物
戒指(化学)
材料科学
有机化学
作者
Akira Mizuno,Kouhei Matsui,Satoshi Shuto
标识
DOI:10.1002/chem.201702119
摘要
Peptidomimetics, non-natural mimicries of bioactive peptides, comprise an important class of drug molecules. The essence of the peptidomimetic design is to mimic the key conformation assumed by the bioactive peptides upon binding to their targets. Regulation of the conformation of peptidomimetics is important not only to enhance target binding affinity and selectivity, but also to confer cell-membrane permeability for targeting protein-protein interactions in cells. The rational design of peptidomimetics with suitable three-dimensional structures is challenging, however, due to the inherent flexibility of peptides and their dynamic conformational changes upon binding to the target biomolecules. In this Minireview, a three-dimensional structural diversity-oriented strategy based on the characteristic structural features of cyclopropane to address this challenging issue in peptidomimetic chemistry is described.
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