Abstract
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.
MeSH terms
-
Adipocytes / metabolism*
-
Amino Acid Sequence / genetics
-
Binding Sites / physiology
-
Carrier Proteins / antagonists & inhibitors*
-
Carrier Proteins / genetics
-
Carrier Proteins / metabolism
-
Diabetes Mellitus, Type 2 / drug therapy*
-
Diabetes Mellitus, Type 2 / metabolism
-
Drug Delivery Systems / methods*
-
Fatty Acid-Binding Proteins
-
Fatty Acids / administration & dosage*
-
Fatty Acids / chemical synthesis*
-
Fatty Acids / metabolism
-
Humans
-
Molecular Sequence Data
Substances
-
Carrier Proteins
-
FABP5 protein, human
-
Fatty Acid-Binding Proteins
-
Fatty Acids