Shutting down the pore: The search for small molecule inhibitors of the mitochondrial permeability transition.


`ileikyt, Justina; Forte, Michael

Publication Year 2016
Journal Biochimica et Biophysica Acta
Pages 1197-1202
Volume 1857
Issue 8
PMID 26924772.0
PMCID PMC4893955
DOI 10.1016/j.bbabio.2016.02.016

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. Copyright ? 2016 Elsevier B.V. All rights reserved.