Discovery of inhibitors of human adipocyte fatty acid-binding protein, a potential type 2 diabetes target
2004; Elsevier BV; Volume: 14; Issue: 17 Linguagem: Inglês
10.1016/j.bmcl.2004.06.057
ISSN1464-3405
AutoresFredrik Lehmann, Saba Haile, Eva Axén, Carmen Medina, J. Uppenberg, Stefan Svensson, Thomas Lundbäck, L Rondahl, Tjeerd Barf,
Tópico(s)Adipose Tissue and Metabolism
ResumoLow 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.
Referência(s)