Rational design of the first small-molecule antagonists of NHERF1/EBP50 PDZ domains

被引：31
作者：
Mayasundari, Anand [1 ]
Ferreira, Antonio M. [2 ]
He, Liwen [1 ]
Mahindroo, Neeraj [1 ]
Bashford, Don [2 ]
Fujii, Naoaki [1 ]
机构：
[1] St Jude Childrens Res Hosp, Dept Chem Biol & Therapeut, Memphis, TN 38105 USA
[2] St Jude Childrens Res Hosp, Hartwell Ctr Bioinformat & Biotechnol, Dept Biol Struct, Memphis, TN 38105 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2008年 / 18卷 / 03期
关键词：
NHERF1; EBP50; PDZ domain; protein-protein interaction inhibitor; indole; small molecule; EXCHANGER REGULATORY FACTOR; TRANSMEMBRANE CONDUCTANCE REGULATOR; GROWTH-FACTOR RECEPTORS; CLASS IPDZ DOMAINS; BETA(2)-ADRENERGIC RECEPTOR; BREAST-CANCER; CELL-GROWTH; PROTEIN; ASSOCIATION; NHERF;
D O I：
10.1016/j.bmcl.2007.12.038
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
This report describes the first small-molecule antagonists that specifically target the ligand-binding pocket of PDZ domains of NHERF1 multi-functional adaptor protein. Comparison of the peptide sequence homology between the native ligand of NHERF1 PDZ domains and an indole-based non-peptide chemical scaffold allowed the design of a small-molecule antagonist of NHERF1 PDZ domains. (C) 2007 Elsevier Ltd. All rights reserved.
引用
收藏
页码：942 / 945
页数：4
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