将甲基替换为三氟甲基是提高短肽膜通透性的一种策略。

Methyl to trifluoromethyl substitution as a strategy to increase the membrane permeability of short peptides.

机构信息

Department of Chemistry & Biotechnology, Graduate School of Engineering, The University of Tokyo, Bunkyo-ku, Tokyo 113-8656, Japan.

Material Integration Laboratories, Yokohama Technical Center, AGC Inc., Yokohama 230-0045, Japan.

出版信息

Org Biomol Chem. 2021 Nov 10;19(43):9386-9389. doi: 10.1039/d1ob01565f.

DOI:10.1039/d1ob01565f

PMID:34676842

Abstract

Here, we investigated the effect of CH to CF substitution on the membrane permeability of peptides. We synthesized a series of peptides with CF groups and corresponding nonfluorinated peptides and measured the membrane permeability of the peptides. As a result, we demonstrated that CH to CF substitution is useful for increasing the membrane permeability of di-/tri-peptides.

摘要

在这里，我们研究了 CH 到 CF 取代对肽的膜通透性的影响。我们合成了一系列具有 CF 基团的肽和相应的非氟化肽，并测量了这些肽的膜通透性。结果表明，CH 到 CF 取代对于提高二肽/三肽的膜通透性是有用的。