Šileikytė Justina, Forte Michael
Department of Biomedical Sciences, University of Padova, Padova I-35131, Italy.
Vollum Institute, Oregon Health & Science University, Portland, OR 97239, USA.
Biochim Biophys Acta. 2016 Aug;1857(8):1197-1202. doi: 10.1016/j.bbabio.2016.02.016. Epub 2016 Feb 26.
The mitochondrial permeability transition pore (PTP) is now recognized as playing a key role in a wide variety of human diseases whose common pathology may be based in mitochondrial dysfunction. Recently, PTP assays have been adapted to high-throughput screening approaches to identify small molecules specifically inhibiting the PTP. Following extensive secondary chemistry, the most potent inhibitors of the PTP described to date have been developed. This review will provide an overview of each of these screening efforts, use of resulting compounds in animal models of PTP-based diseases, and problems that will require further study. This article is part of a Special Issue entitled 'EBEC 2016: 19th European Bioenergetics Conference, Riva del Garda, Italy, July 2-6, 2016', edited by Prof. Paolo Bernardi.
线粒体通透性转换孔（PTP）现已被公认为在多种人类疾病中起关键作用，这些疾病的共同病理可能基于线粒体功能障碍。最近，PTP检测已适用于高通量筛选方法，以鉴定特异性抑制PTP的小分子。经过广泛的二次化学研究，迄今已开发出最有效的PTP抑制剂。本综述将概述这些筛选工作中的每一项、所得化合物在基于PTP疾病的动物模型中的应用，以及需要进一步研究的问题。本文是由Paolo Bernardi教授编辑的特刊“EBEC 2016：第19届欧洲生物能学会议，意大利里瓦加尔达，2016年7月2日至6日”的一部分。
