3G9E

Aleglitaar. a new. potent, and balanced dual ppara/g agonist for the treatment of type II diabetes

3G9E の概要

• エントリーDOI: 10.2210/pdb3g9e/pdb
• 関連するPDBエントリー: 3G8I
• 分子名称: Peroxisome proliferator-activated receptor gamma, Nuclear receptor coactivator 1, (2S)-2-methoxy-3-{4-[2-(5-methyl-2-phenyl-1,3-oxazol-4-yl)ethoxy]-1-benzothiophen-7-yl}propanoic acid, ... (4 entities in total)
• 機能のキーワード: nuclear receptor, transcription factor, diabetes, activator, alternative splicing, diabetes mellitus, disease mutation, dna-binding, metal-binding, nucleus, obesity, phosphoprotein, polymorphism, receptor, transcription, transcription regulation, zinc, zinc-finger, acyltransferase, chromosomal rearrangement, proto-oncogene, transferase, ubl conjugation, transcription-transferase complex, transcription/transferase
• 由来する生物種: Homo sapiens (Human); 詳細
• 細胞内の位置: Nucleus: P37231; Nucleus (By similarity): Q15788
• タンパク質・核酸の鎖数: 2
• 化学式量合計: 32906.23

構造登録者

Ruf, A.,Benz, J.,Bernardeau, A.,Binggeli, A.,Blum, D.,Boehringer, M.,Grether, U.,Hilpert, H.,Kuhn, B.,Maerki, H.P.,Meyer, M.,Puenterner, K.,Raab, S.,Schlatter, D.,Gsell, B.,Stihle, M.,Mohr, P. (登録日: 2009-02-13, 公開日: 2009-06-02, 最終更新日: 2023-11-01)

主引用文献

Benardeau, A.,Benz, J.,Binggeli, A.,Blum, D.,Boehringer, M.,Grether, U.,Hilpert, H.,Kuhn, B.,Marki, H.P.,Meyer, M.,Puntener, K.,Raab, S.,Ruf, A.,Schlatter, D.,Mohr, P.
Aleglitazar, a new, potent, and balanced dual PPARalpha/gamma agonist for the treatment of type II diabetes.
Bioorg.Med.Chem.Lett., 19:2468-2473, 2009

PubMed Abstract: Design, synthesis, and SAR of novel alpha-alkoxy-beta-arylpropionic acids as potent and balanced PPARalphagamma coagonists are described. One representative thereof, Aleglitazar ((S)-2Aa), was chosen for clinical development. Its X-ray structure in complex with both receptors as well as its high efficacy in animal models of T2D and dyslipidemia are also presented.

PubMed: 19349176
DOI: 10.1016/j.bmcl.2009.03.036

実験手法

X-RAY DIFFRACTION (2.3 Å)