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2OW3

Glycogen synthase kinase-3 beta in complex with bis-(indole)maleimide pyridinophane inhibitor

2OW3 の概要
エントリーDOI10.2210/pdb2ow3/pdb
分子名称Glycogen synthase kinase-3 beta, BIS-(INDOLE)MALEIMIDE PYRIDINOPHANE (3 entities in total)
機能のキーワードkinase-inhibitor complex, transferase
由来する生物種Homo sapiens (human)
細胞内の位置Cytoplasm : P49841
タンパク質・核酸の鎖数2
化学式量合計81251.28
構造登録者
Zhang, H.C.,Bonaga, L.V.,Ye, H.,Derian, C.K.,Damiano, B.P.,Maryanoff, B.E. (登録日: 2007-02-15, 公開日: 2008-02-19, 最終更新日: 2024-11-13)
主引用文献Zhang, H.C.,Bonaga, L.V.,Ye, H.,Derian, C.K.,Damiano, B.P.,Maryanoff, B.E.
Novel bis(indolyl)maleimide pyridinophanes that are potent, selective inhibitors of glycogen synthase kinase-3.
Bioorg.Med.Chem.Lett., 17:2863-2868, 2007
Cited by
PubMed Abstract: Novel bis(indolyl)maleimide pyridinophanes 3, 9a, 9b, 10a, 10b, and 11 were prepared by cobalt-mediated [2+2+2] cycloaddition of an appropriate alpha,omega-diyne with an N,N-dialkylcyanamide. These macrocyclic heterophanes were found to be potent, selective inhibitors of glycogen synthase kinase-3beta. An X-ray structure of a co-crystal of GSK-3beta and 3 (IC(50)=3nM) depicts the hydrogen bonding and hydrophobic interactions in the ATP-binding pocket of this serine/threonine protein kinase.
PubMed: 17350261
DOI: 10.1016/j.bmcl.2007.02.059
主引用文献が同じPDBエントリー
実験手法
X-RAY DIFFRACTION (2.8 Å)
構造検証レポート
Validation report summary of 2ow3
検証レポート(詳細版)ダウンロードをダウンロード

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件を2024-12-18に公開中

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