3QCX

Phosphoinositide-Dependent Kinase-1 (PDK1) kinase domain with 6-{2-Amino-6-[(3R)-3-methyl-4-morpholinyl]-4-pyrimidinyl}-1H-indazol-3-amine

3QCX の概要

• エントリーDOI: 10.2210/pdb3qcx/pdb
• 関連するPDBエントリー: 3NUN 3NUS 3NUU 3NUY 3QCQ 3QCS 3QCY 3QD0 3QD3 3QD4
• 分子名称: 3-phosphoinositide-dependent protein kinase 1, GLYCEROL, SULFATE ION, ... (5 entities in total)
• 機能のキーワード: kinase domain, agc kinase, signal transduction, phosphorylation on s241, transferase-transferase inhibitor complex, transferase/transferase inhibitor
• 由来する生物種: Homo sapiens (human)
• 細胞内の位置: Cytoplasm: O15530
• タンパク質・核酸の鎖数: 1
• 化学式量合計: 37015.07

構造登録者

Medina, J.R.,Becker, C.J.,Blackledge, C.W.,Duquenne, C.,Feng, Y.,Grant, S.W.,Heerding, D.,Li, W.H.,Miller, W.H.,Romeril, S.P.,Scherzer, D.,Shu, A.,Bobko, M.A.,Chadderton, A.R.,Dumble, M.,Gradiner, C.M.,Gilbert, S.,Liu, Q.,Rabindran, S.K.,Sudakin, V.,Xiang, H.,Brady, P.G.,Campobasso, N.,Ward, P.,Axten, J.M. (登録日: 2011-01-17, 公開日: 2011-03-09, 最終更新日: 2011-11-16)

• 主引用文献: Medina, J.R.,Becker, C.J.,Blackledge, C.W.,Duquenne, C.,Feng, Y.,Grant, S.W.,Heerding, D.,Li, W.H.,Miller, W.H.,Romeril, S.P.,Scherzer, D.,Shu, A.,Bobko, M.A.,Chadderton, A.R.,Dumble, M.,Gardiner, C.M.,Gilbert, S.,Liu, Q.,Rabindran, S.K.,Sudakin, V.,Xiang, H.,Brady, P.G.,Campobasso, N.,Ward, P.,Axten, J.M.; Structure-Based Design of Potent and Selective 3-Phosphoinositide-Dependent Kinase-1 (PDK1) Inhibitors.; J.Med.Chem., 54:1871-1895, 2011; PubMed: 21341675; DOI: 10.1021/jm101527u

実験手法

X-RAY DIFFRACTION (2.3 Å)