Abstract
We first identified fluorescein, ketazolam, antrafenine, darifenacin, fosaprepitant, paliperidone, risperidone, pimozide, trovafloxacin, and levofloxacin as inhibitors of fatty acid binding protein 4 using molecular docking screening from FDA-approved drugs. Subsequently, the biochemical characterizations showed that levofloxacin directly inhibited FABP4 activity in both the in vitro ligand displacement assay and cell-based function assay. Furthermore, levofloxacin did not induce adipogenesis in adipocytes, which is the major adverse effect of FABP4 inhibitors.
Publication types
-
Letter
-
Research Support, Non-U.S. Gov't
MeSH terms
-
Drug Approval
-
Drug Discovery*
-
Fatty Acid-Binding Proteins / antagonists & inhibitors*
-
Fatty Acid-Binding Proteins / chemistry
-
Fatty Acid-Binding Proteins / metabolism*
-
Humans
-
Ligands
-
Metabolic Diseases / drug therapy
-
Molecular Docking Simulation*
-
Protein Conformation
-
Small Molecule Libraries / metabolism*
-
Small Molecule Libraries / pharmacology*
-
Small Molecule Libraries / therapeutic use
-
United States
-
United States Food and Drug Administration*
Substances
-
FABP4 protein, human
-
Fatty Acid-Binding Proteins
-
Ligands
-
Small Molecule Libraries