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

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.

• Authors: Giuseppe Floresta, Venerando Pistarà, Emanuele Amata, Maria Dichiara, Agostino Marrazzo, Orazio Prezzavento, Antonio Rescifina
• Journal: European journal of medicinal chemistry (Eur J Med Chem) Vol. 138 Pg. 854-873 (Sep 29 2017) ISSN: 1768-3254 [Electronic] France
• PMID: 28738306 (Publication Type: Journal Article, Review, Systematic Review)
• Copyright: Copyright © 2017 Elsevier Masson SAS. All rights reserved.

Chemical References

• FABP4 protein, human
• Fatty Acid-Binding Proteins
• Small Molecule Libraries

Topics

• Dose-Response Relationship, Drug
• Fatty Acid-Binding Proteins (antagonists & inhibitors)
• Humans
• Molecular Structure
• Small Molecule Libraries (chemistry, pharmacology)
• Structure-Activity Relationship