Arylamide derivatives as peptidomimetic inhibitors of calmodulin

被引：32

作者：

Yin, H ^{[1
]}

Frederick, KK ^{[1
]}

Liu, DH ^{[1
]}

Wand, AJ ^{[1
]}

DeGrado, WF ^{[1
]}

机构：

[1] Univ Penn, Sch Med, Dept Biochem & Biophys, Philadelphia, PA 19104 USA

来源：

ORGANIC LETTERS | 2006年 / 8卷 / 02期

关键词：

D O I：

10.1021/ol052478j

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

Many peptides bind to calmodulin (CaM) in a helical conformation. Here we describe a group of synthetic inhibitors of CaM based on an arylamide scaffold that is intended to mimic smMLCK, a CaM-binding helical peptide. Compound 1 showed a K-i value of 7.10 +/- 1.48 nM in a fluorescence polarization assay that monitors the strong association of CaM and its peptide ligand mastoparan X. (H-1,N-15)-HSQC NMR spectroscopy experiments suggested that 1 binds to CaM in an analogous fashion to that of smMLCK.

引用

页码：223 / 225

页数：3

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