5AZT

Ternary complex of hPPARalpha ligand binding domain, 17-oxoDHA and a SRC1 peptide

5AZT の概要

• エントリーDOI: 10.2210/pdb5azt/pdb
• 関連するPDBエントリー: 5AZV
• 分子名称: Peroxisome proliferator-activated receptor alpha, 15-meric peptide from Nuclear receptor coactivator 1, (4~{Z},7~{Z},10~{Z},13~{Z},19~{Z})-17-oxidanylidenedocosa-4,7,10,13,19-pentaenoic acid, ... (4 entities in total)
• 機能のキーワード: nuclear receptor, transcription regulation, ligand binding domain, zinc-finger, dna binding, transcription, obesity, nucleus, receptor, activator, oxidized fatty acid, transcription factor, agonist, dual agonist, covalent, ppre, nuclear, co-activator, dna binding protein
• 由来する生物種: Homo sapiens (Human); 詳細
• タンパク質・核酸の鎖数: 3
• 化学式量合計: 63266.19

構造登録者

Egawa, D.,Itoh, T.,Yamamoto, K. (登録日: 2015-10-23, 公開日: 2016-07-06, 最終更新日: 2024-10-30)

主引用文献

Egawa, D.,Itoh, T.,Akiyama, Y.,Saito, T.,Yamamoto, K.
17-OxoDHA Is a PPAR alpha/gamma Dual Covalent Modifier and Agonist
Acs Chem.Biol., 2016

PubMed 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.

PubMed: 27337155
DOI: 10.1021/acschembio.6b00338

実験手法

X-RAY DIFFRACTION (3.45 Å)