小分子线粒体解偶联剂及其治疗潜力。
Small Molecule Mitochondrial Uncouplers and Their Therapeutic Potential.
机构信息
Department of Chemistry and Virginia Tech Center for Drug Discovery , Virginia Tech , Blacksburg , Virginia 24061 , United States.
School of Biotechnology and Biomolecular Sciences , University of New South Wales , Kensington , NSW 2033 , Australia.
出版信息
J Med Chem. 2018 Jun 14;61(11):4641-4655. doi: 10.1021/acs.jmedchem.7b01182. Epub 2017 Dec 8.
Small molecule mitochondrial uncouplers transport protons from the mitochondrial inner membrane space into the mitochondrial matrix independent of ATP synthase, uncoupling nutrient metabolism from ATP generation. The therapeutic potential of mitochondrial uncouplers has been investigated for the treatment of metabolic diseases such as obesity and type 2 diabetes (T2D), ischemia-reperfusion injury, and neurodegenerative diseases. This communication will review the small molecule mitochondrial uncouplers reported to date and explore their potential as therapeutics.
小分子线粒体解偶联剂可将质子从线粒体膜间隙转运到线粒体基质中，而不依赖于 ATP 合酶，从而将营养代谢与 ATP 生成解偶联。线粒体解偶联剂的治疗潜力已在肥胖和 2 型糖尿病 (T2D)、缺血再灌注损伤和神经退行性疾病等代谢性疾病的治疗中进行了研究。本通讯将回顾迄今为止报道的小分子线粒体解偶联剂，并探讨它们作为治疗剂的潜力。
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