Discovery of inhibitors of human adipocyte fatty acid-binding protein, a potential type 2 diabetes target

被引：73

作者：

Lehmann, F

Haile, S

Axen, E

Medina, C

Uppenberg, J

Svensson, S

Lundbäck, T

Rondahl, L

Barf, T ^{[1
]}

机构：

[1] Biovitrum AB, Dept Med Chem, SE-75137 Uppsala, Sweden

[2] Biovitrum AB, Dept Assay Dev & Screening, SE-75137 Uppsala, Sweden

[3] Biovitrum AB, Dept Struct Chem, SE-75137 Uppsala, Sweden

[4] Biovitrum AB, Dept Biol, SE-75137 Uppsala, Sweden

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 17期

关键词：

A-FABP inhibitors; FABP4;

D O I：

10.1016/j.bmcl.2004.06.057

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Low micromolar human A-FABP inhibitors were found by utilizing a fluorescence polarization assay, X-ray crystallography and modeling. The carbazole- and indole-based inhibitors displayed approximately 10-fold preferences over human H-FABP and E-FABP, and are highly selective against I-FABP. This communication describes the SAR for drug-like synthetic inhibitors of human A-FABP. (C) 2004 Elsevier Ltd. All rights reserved.

引用

页码：4445 / 4448

页数：4

共 18 条

[1] ICM - A NEW METHOD FOR PROTEIN MODELING AND DESIGN - APPLICATIONS TO DOCKING AND STRUCTURE PREDICTION FROM THE DISTORTED NATIVE CONFORMATION [J].