1tow

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1tow, resolution 2.00Å

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Crystal structure of human adipocyte fatty acid binding protein in complex with a carboxylic acid ligand

Overview

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.

About this Structure

1TOW is a Single protein structure of sequence from Homo sapiens with CRZ as ligand. Full crystallographic information is available from OCA.

Reference

Discovery of inhibitors of human adipocyte fatty acid-binding protein, a potential type 2 diabetes target., Lehmann F, Haile S, Axen E, Medina C, Uppenberg J, Svensson S, Lundback T, Rondahl L, Barf T, Bioorg Med Chem Lett. 2004 Sep 6;14(17):4445-8. PMID:15357969

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