螺旋-环-螺旋肽折叠体及其在水解酶模拟物构建中的应用。

Helix-loop-helix peptide foldamers and their use in the construction of hydrolase mimetics.

机构信息

Department of Bioorganic Chemistry, Wrocław University of Science and Technology, Wybrzeże Wyspiańskiego 27, 50-370 Wrocław, Poland.

Amsterdam Machine Learning Lab, University of Amsterdam, Science Park 904, 1098 XH Amsterdam, The Netherlands.

出版信息

Bioorg Chem. 2018 Dec;81:356-361. doi: 10.1016/j.bioorg.2018.07.012. Epub 2018 Jul 17.

DOI:10.1016/j.bioorg.2018.07.012

PMID:30195249

Abstract

De novo designed helix-loop-helix peptide foldamers containing cis-2-aminocyclopentanecarboxylic acid residues were evaluated for their conformational stability and possible use in enzyme mimetic development. The correlation between hydrogen bond network size and conformational stability was demonstrated through CD and NMR spectroscopies. Molecules incorporating a Cys/His/Glu triad exhibited enzyme-like hydrolytic activity.

摘要

从头设计的含有顺式-2-氨基环戊烷羧酸残基的螺旋环螺旋肽类折叠物，用于评估其构象稳定性和在酶模拟开发中的可能用途。通过 CD 和 NMR 光谱学证明了氢键网络大小与构象稳定性之间的相关性。包含 Cys/His/Glu 三联体的分子表现出类似酶的水解活性。