| Literature DB >> 27855359 |
TaeHun Kim1, Ha Yun Yang2, Beoung Gun Park3, Seo Yun Jung3, Jong-Hyun Park3, Ki Duk Park1, Sun-Joon Min4, Jinsung Tae5, Hyejin Yang6, Suengmok Cho6, Sung Jin Cho7, Hyundong Song8, Inhee Mook-Jung8, Jiyoun Lee9, Ae Nim Pae10.
Abstract
In this study, we designed a library of compounds based on the structures of well-known ligands of the 18 kDa translocator protein (TSPO), one of the putative components of the mPTP. We performed diverse mitochondrial functional assays to assess their ability to restore cells from Aβ-induced toxicity in vitro and in vivo. Among tested compounds, compound 25 effectively improved cognitive function in animal models of AD. Given the excellent in vitro and in vivo activity and a favorable pharmacokinetic profile of compound 25, we believe that it can serve as a promising lead compound for a potential treatment option for AD. Copyright ÂEntities:
Keywords: Alzheimer's disease; Aβ; Mitochondrial dysfunction; Mitochondrial permeability transition pore; TSPO; Translocator protein
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Year: 2016 PMID: 27855359 DOI: 10.1016/j.ejmech.2016.11.017
Source DB: PubMed Journal: Eur J Med Chem ISSN: 0223-5234 Impact factor: 6.514