Discovery of highly selective inhibitors of human fatty acid binding protein 4 (FABP4) by virtual screening

Compound 1 was identified as an inhibitor of human FABP4 with an IC50 of 13.5μM and it showed a selectivity more than 144-fold over human FABP3. In this study, a series of small molecule inhibitors of human FABP4 were identified through virtual screening. Compound 1 is the most potent hit against FA...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2010-06, Vol.20 (12), p.3675-3679
Hauptverfasser:	Cai, Haiyan, Yan, Guirui, Zhang, Xiaodong, Gorbenko, Olena, Wang, Heyao, Zhu, Weiliang
Format:	Artikel
Sprache:	eng
Schlagworte:	Atherosclerosis - drug therapy Binding Sites Biological and medical sciences Cardiovascular system Computer Simulation Diabetes Mellitus - drug therapy Drug Discovery Drug Evaluation, Preclinical - methods FABP3 FABP4 Fatty Acid Binding Protein 3 Fatty Acid-Binding Proteins - antagonists & inhibitors Fatty Acid-Binding Proteins - chemistry Fatty Acid-Binding Proteins - genetics General and cellular metabolism. Vitamins Humans Inhibitor MD studies Medical sciences Miscellaneous Mutation Obesity - drug therapy Organic Chemicals - chemistry Organic Chemicals - pharmacology Pharmacology. Drug treatments Protein Binding - genetics Selectivity Structure-Activity Relationship Substrate Specificity
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