2NPA

the crystal structure of the human PPARaplpha ligand binding domain in complex with a a-hydroxyimino phenylpropanoic acid

2NPA の概要

• エントリーDOI: 10.2210/pdb2npa/pdb
• 分子名称: Peroxisome proliferator-activated receptor alpha, SRC- peptide from Nuclear receptor coactivator 1, (2R,3E)-2-{4-[(5-METHYL-2-PHENYL-1,3-OXAZOL-4-YL)METHOXY]BENZYL}-3-(PROPOXYIMINO)BUTANOIC ACID, ... (4 entities in total)
• 機能のキーワード: protein-agonist complex, transcription
• 由来する生物種: Homo sapiens (human); 詳細
• 細胞内の位置: Nucleus: Q07869
• タンパク質・核酸の鎖数: 4
• 化学式量合計: 65596.55

構造登録者

Kim, K.H.,Chung, H.K.,Han, H.O.,Kim, S.H.,Koh, J.S.,Kim, G.T. (登録日: 2006-10-26, 公開日: 2007-10-30, 最終更新日: 2023-10-25)

主引用文献

Han, H.O.,Kim, S.H.,Kim, K.H.,Hur, G.C.,Yim, H.J.,Chung, H.K.,Woo, S.H.,Koo, K.D.,Lee, C.S.,Koh, J.S.,Kim, G.T.
Design and synthesis of oxime ethers of alpha-acyl-beta-phenylpropanoic acids as PPAR dual agonists
Bioorg.Med.Chem.Lett., 17:937-941, 2007

PubMed Abstract: Oxime ethers of alpha-acyl-beta-phenylpropanoic acids were prepared to apply as PPARalpha and gamma dual agonists. Among them, compound 11l proved to exhibit potent in vitro activities with EC(50) of 19 and 13nM in PPARalpha and gamma, respectively. It showed better glucose lowering effects than rosiglitazone 1 and ameliorated the lipid profile like plasma triglyceride in db/db mice model.

PubMed: 17157019
DOI: 10.1016/j.bmcl.2006.11.050

実験手法

X-RAY DIFFRACTION (2.3 Å)