期刊
BIOCHIMICA ET BIOPHYSICA ACTA-BIOENERGETICS
卷 1857, 期 8, 页码 1197-1202出版社
ELSEVIER SCIENCE BV
DOI: 10.1016/j.bbabio.2016.02.016
关键词
Mitochondria; Permeability transition; Inhibitors; High-throughput; Screening
资金
- NIGMS NIH HHS [R01 GM069883] Funding Source: Medline
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. (C) 2016 Elsevier B.V. All rights reserved.
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