Small Molecule Inhibitors of Human Adipocyte Fatty Acid Binding Protein (FABP4)

doi:10.2174/15734064113096660045

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	Small Molecule Inhibitors of Human Adipocyte Fatty Acid Binding Protein (FABP4)
	Zhang, Mingming 1; Zhu, Weiliang2 ; Li, Yingxia 1
刊名	MEDICINAL CHEMISTRY
	2014-06
卷号	10 期号:4 页码:339-347
关键词	Fatty acid binding protein 4 FABP4 inhibitor receptor small molecule type 2 diabetes
ISSN号	1573-4064
DOI	10.2174/15734064113096660045
文献子类	Article
英文摘要	Fatty acid binding protein 4 (FABP4) is expressed in adipocytes and macrophages, and modulates inflammatory and metabolic response. Studies in FABP4-deficient mice have shown that this lipid carrier has a significant role within the field of metabolic syndrome, inflammation and atherosclerosis; thus, its inhibition may open up new opportunities to develop novel therapeutic agents. A number of potent small molecule inhibitors of FABP4 have been identified and found to have the potential to prevent and treat metabolic diseases such as type-2 diabetes and atherosclerosis. Due to the ubiquity of endogenous fatty acids and the high intracellular concentration of FABP4, the inhibitors need to have significantly greater intrinsic potency than endogenous fatty acids. Furthermore, heart-type FABP (FABP3), which is expressed in both heart and skeletal muscle, is involved in active fatty acid metabolism where it transports fatty acids from the cell membrane to mitochondria for oxidation. However, FABP3 shares high overall sequence identity and similar 3D structure with FABP4, but has a potential problem with selectivity. In this review, we would like to analyze the main inhibitors that have appeared in the literature in the last decade, focusing on chemical structures, biological properties, selectivity and structure-activity relationships.
资助项目	National High-tech R&D Program of China[2011AA09070105]
WOS关键词	HORMONE-SENSITIVE LIPASE ; ACTIVATED RECEPTOR-GAMMA ; INSULIN-RESISTANCE ; AP2 ; OBESITY ; MICE ; ATHEROSCLEROSIS ; DESIGN ; AFABP ; CELL
WOS研究方向	Pharmacology & Pharmacy
语种	英语
出版者	BENTHAM SCIENCE PUBL LTD
WOS记录号	WOS:000334852400001
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/277062]
专题	药物发现与设计中心
通讯作者	Li, Yingxia
作者单位	1.Fudan Univ, Sch Pharm, Shanghai 201203, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China
推荐引用方式 GB/T 7714	Zhang, Mingming,Zhu, Weiliang,Li, Yingxia. Small Molecule Inhibitors of Human Adipocyte Fatty Acid Binding Protein (FABP4)[J]. MEDICINAL CHEMISTRY,2014,10(4):339-347.
APA	Zhang, Mingming,Zhu, Weiliang,&Li, Yingxia.(2014).Small Molecule Inhibitors of Human Adipocyte Fatty Acid Binding Protein (FABP4).MEDICINAL CHEMISTRY,10(4),339-347.
MLA	Zhang, Mingming,et al."Small Molecule Inhibitors of Human Adipocyte Fatty Acid Binding Protein (FABP4)".MEDICINAL CHEMISTRY 10.4(2014):339-347.