Dipartimento di Scienze del Farmaco e della Salute, Università di Catania, Viale Andrea Doria 6, 95125, Catania, Italy.
Dipartimento di Scienze del Farmaco e della Salute, Università di Catania, Viale Andrea Doria 6, 95125, Catania, Italy.
Eur J Med Chem. 2022 Oct 5;240:114604. doi: 10.1016/j.ejmech.2022.114604. Epub 2022 Jul 14.
The fatty acid binding protein 4 (FABP4) is a protein predominantly expressed in macrophages and adipose tissue, where it regulates fatty acids storage and lipolysis and is an essential mediator of inflammation. Small molecule inhibitors of FABP4 have attracted interest following the recent publications of beneficial pharmacological effects of these compounds for the treatment of metabolic syndrome and, more recently, for other pathologies. Since the synthesis of the BMS309403, one of the first selective and effective FABP4 inhibitors, hundreds of other inhibitors have been synthesized (i.e., derivatives of niacin, quinoxaline, aryl-quinoline, bicyclic pyridine, urea, aromatic compounds and other novel heterocyclic compounds). This review updates the recently reported (2017 to early 2022) molecules as adipocyte fatty acid binding protein 4 inhibitors.
脂肪酸结合蛋白 4（FABP4）是一种主要在巨噬细胞和脂肪组织中表达的蛋白质，它调节脂肪酸的储存和脂肪分解，是炎症的重要介质。最近有文献报道，小分子 FABP4 抑制剂对代谢综合征和最近对其他疾病的治疗具有有益的药理作用，因此引起了人们的兴趣。自从合成第一种选择性和有效的 FABP4 抑制剂 BMS309403 以来，已经合成了数百种其他抑制剂（即烟酸、喹喔啉、芳基喹啉、双环吡啶、脲、芳香族化合物和其他新型杂环化合物的衍生物）。本综述更新了最近报道的（2017 年至 2022 年初）作为脂肪细胞脂肪酸结合蛋白 4 抑制剂的分子。
