| Literature DB >> 27337155 |
Daichi Egawa1, Toshimasa Itoh1, Yui Akiyama1, Tomoko Saito1, Keiko Yamamoto1.
Abstract
17-Hydroxy docosahexaenoic acid (17-HDHA) is an oxidized form of docosahexaenoic acid (DHA) and known as a specialized proresolving mediator. We found that a further oxidized product, 17-oxodocosahexaenoic acid (17-oxoDHA), activates peroxisome proliferator-activated receptors γ (PPARγ) and PPARα in transcriptional assays and thus can be classified as an α/γ dual agonist. ESI mass spectroscopy and X-ray crystallographic analysis showed that 17-oxoDHA binds to PPARγ and PPARα covalently, making 17-oxoDHA the first of a novel class of PPAR agonists, the PPARα/γ dual covalent agonist. Furthermore, the covalent binding sites were identified as Cys285 for PPARγ and Cys275 for PPARα.Entities:
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Year: 2016 PMID: 27337155 DOI: 10.1021/acschembio.6b00338
Source DB: PubMed Journal: ACS Chem Biol ISSN: 1554-8929 Impact factor: 5.100