Discovery of inhibitors of human adipocyte fatty acid-binding protein, a potential type 2 diabetes target.

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Lehmann F, Haile S, Axen E, Medina C, Uppenberg J, Svensson S, Lundback T, Rondahl L, Barf T

Discovery of inhibitors of human adipocyte fatty acid-binding protein, a potential type 2 diabetes target.

Bioorg Med Chem Lett. 2004 Sep 6;14(17):4445-8.

PubMed ID
15357969 [ View in PubMed
]
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.

DrugBank Data that Cites this Article

Polypeptides
NameUniProt ID
Fatty acid-binding protein, adipocyteP15090Details
Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
Carbazole Butanoic AcidFatty acid-binding protein, adipocyteIC 50 (nM)570N/AN/ADetails
Palmitic AcidFatty acid-binding protein, adipocyteIC 50 (nM)930N/AN/ADetails
Palmitic AcidFatty acid-binding protein, epidermalIC 50 (nM)1200N/AN/ADetails
Palmitic AcidFatty acid-binding protein, heartIC 50 (nM)2600N/AN/ADetails
Palmitic AcidFatty acid-binding protein, intestinalIC 50 (nM)1700N/AN/ADetails