National Center for
1TOW: Crystal Structure Of Human Adipocyte Fatty Acid Binding Protein In Complex With A Carboxylic Acid Ligand
Discovery of inhibitors of human adipocyte fatty acid-binding protein, a potential type 2 diabetes target
Bioorg. Med. Chem. Lett. (2004) 14 p.4445-4448
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.