4MPN

Crystal structure of pyruvate dehydrogenase kinase isoform 2 in complex with inhibitor PS10

4MPN の概要

• エントリーDOI: 10.2210/pdb4mpn/pdb
• 関連するPDBエントリー: 4MP2 4MP7 4MPC 4MPE
• 分子名称: [Pyruvate dehydrogenase [lipoamide]] kinase isozyme 2, mitochondrial, 2-[(2,4-dihydroxyphenyl)sulfonyl]-2,3-dihydro-1H-isoindole-4,6-diol, L(+)-TARTARIC ACID, ... (4 entities in total)
• 機能のキーワード: ghkl protein kinase, pyruvate dehydrogenase complex, mitochondrial protein kinases, impaired glucose oxidation, hepatic steatosis, type 2 diabetes, cancer, bergerat nucleotide-binding fold, protein kinase, transferase
• 由来する生物種: Homo sapiens (human)
• 細胞内の位置: Mitochondrion matrix: Q15119
• タンパク質・核酸の鎖数: 1
• 化学式量合計: 45706.81

構造登録者

Gui, W.J.,Tso, S.C.,Chuang, J.L.,Wu, C.Y.,Qi, X.,Tambar, U.K.,Wynn, R.M.,Chuang, D.T. (登録日: 2013-09-13, 公開日: 2014-01-01, 最終更新日: 2024-02-28)

• 主引用文献: Tso, S.C.,Qi, X.,Gui, W.J.,Wu, C.Y.,Chuang, J.L.,Wernstedt-Asterholm, I.,Morlock, L.K.,Owens, K.R.,Scherer, P.E.,Williams, N.S.,Tambar, U.K.,Wynn, R.M.,Chuang, D.T.; Structure-guided Development of Specific Pyruvate Dehydrogenase Kinase Inhibitors Targeting the ATP-binding Pocket.; J.Biol.Chem., 289:4432-4443, 2014; PubMed: 24356970; DOI: 10.1074/jbc.M113.533885

実験手法

X-RAY DIFFRACTION (1.752 Å)