靶向脂肪甘油三酯脂肪酶的小分子抑制剂的研发。
Development of small-molecule inhibitors targeting adipose triglyceride lipase.
机构信息
Institute of Organic Chemistry, Graz University of Technology, 8010 Graz, Austria.
Institute of Molecular Biosciences, University of Graz, 8010 Graz, Austria.
出版信息
Nat Chem Biol. 2013 Dec;9(12):785-7. doi: 10.1038/nchembio.1359. Epub 2013 Oct 6.
Adipose triglyceride lipase (ATGL) is rate limiting in the mobilization of fatty acids from cellular triglyceride stores. This central role in lipolysis marks ATGL as an interesting pharmacological target as deregulated fatty acid metabolism is closely linked to dyslipidemic and metabolic disorders. Here we report on the development and characterization of a small-molecule inhibitor of ATGL. Atglistatin is selective for ATGL and reduces fatty acid mobilization in vitro and in vivo.
脂肪甘油三酯脂肪酶 (ATGL) 在从细胞内甘油三酯储存中动员脂肪酸方面起着限速作用。在脂肪分解中发挥的核心作用使 ATGL 成为一个有趣的药理学靶点，因为脂肪酸代谢失调与血脂异常和代谢紊乱密切相关。本文报道了一种 ATGL 小分子抑制剂的开发和特性。Atglistatin 对 ATGL 具有选择性，可减少体外和体内的脂肪酸动员。
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