Adipocyte fatty acid binding protein 4 (FABP4) inhibitors. A comprehensive systematic review.

Giuseppe Floresta, Venerando Pistarà, Emanuele Amata, Maria Dichiara, Agostino Marrazzo, Orazio Prezzavento, Antonio Rescifina

Journal: European journal of medicinal chemistry 2017;138():854-873

PMID: 28738306

Full Text on Elsevier Science View on PubMed

Abstract

Small molecule inhibitors of adipocyte fatty acid binding protein 4 (FABP4) have attracted interest following the recent publications of beneficial pharmacological effects of these compounds. FABP4 is predominantly expressed in macrophages and adipose tissue where it regulates fatty acids (FAs) storage and lipolysis and is an important mediator of inflammation. In the past years, hundreds FABP4 inhibitors have been synthesized for effective atherosclerosis and diabetes treatments, including derivatives of niacin, quinoxaline, aryl-quinoline, bicyclic pyridine, urea, aromatic compounds and other novel heterocyclic compounds. This review provides an overview of the synthesized and discovered molecules as adipocyte fatty acid binding protein 4 inhibitors (FABP4is) since the synthesis of the putative FABP4i, BMS309403, highlighting the interactions of the different classes of inhibitors with the targets.

Address: Dipartimento di Scienze del Farmaco, Università degli Studi di Catania, V.le A. Doria, 95125 Catania, Italy; Dipartimento di Scienze Chimiche, Università degli Studi di Catania, V.le A. Doria, 95125 Catania, Italy. Electronic address: [email protected].; Dipartimento di Scienze del Farmaco, Università degli Studi di Catania, V.le A. Doria, 95125 Catania, Italy.; Dipartimento di Scienze del Farmaco, Università degli Studi di Catania, V.le A. Doria, 95125 Catania, Italy. Electronic address: [email protected].

DOI: 10.1016/j.ejmech.2017.07.022