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线粒体通透性转换孔:神经退行性变的潜在药物靶点。

Mitochondrial permeability transition pore: a potential drug target for neurodegeneration.

机构信息

Department of Pharmacology and Toxicology, Higuchi Bioscience Center, School of Pharmacy, University of Kansas, Lawrence, KS 66047, USA.

Department of Pharmacology and Toxicology, Higuchi Bioscience Center, School of Pharmacy, University of Kansas, Lawrence, KS 66047, USA.

出版信息

Drug Discov Today. 2018 Dec;23(12):1983-1989. doi: 10.1016/j.drudis.2018.08.001. Epub 2018 Aug 3.

Abstract

The mitochondrial permeability transition pore (mPTP) has been considered a key contributor to cell death, inducing the process in several major neurodegenerative diseases. To date, the molecular nature of the mPTP remains confounding but its significance is universally acknowledged. Several targets have been screened and inhibition of mPTP has emerged as an attractive field for researchers. Nowadays, in silico-directed studies help to explore new small molecules targeting the mPTP to improve their drug-like properties and bioactivity. Here, we briefly summarize the role of mPTP in neurodegenerative diseases, including Alzheimer's disease (AD), Parkinson disease (PD), and Huntington's disease (HD), and discusses current and future potential therapeutic targets.

摘要

线粒体通透性转换孔(mPTP)被认为是细胞死亡的关键贡献者,它在几种主要的神经退行性疾病中诱导了这一过程。迄今为止,mPTP 的分子性质仍然令人困惑,但它的重要性是普遍公认的。已经筛选了几个靶点,mPTP 的抑制作用已经成为研究人员关注的一个有吸引力的领域。如今,基于计算机的研究有助于探索针对 mPTP 的新小分子,以改善它们的类药性和生物活性。在这里,我们简要总结了 mPTP 在神经退行性疾病中的作用,包括阿尔茨海默病(AD)、帕金森病(PD)和亨廷顿病(HD),并讨论了当前和未来的潜在治疗靶点。

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