4EZK

Potent and Selective Inhibitors of PI3K-delta: Obtaining Isoform Selectivity from the Affinity Pocket and Tryptophan Shelf

4EZK の概要

• エントリーDOI: 10.2210/pdb4ezk/pdb
• 関連するPDBエントリー: 4EZJ 4EZL
• 分子名称: Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform, 2-(1-{[2-(2H-indazol-4-yl)-4-(morpholin-4-yl)pyrido[3,2-d]pyrimidin-6-yl]methyl}piperidin-4-yl)propan-2-ol (3 entities in total)
• 機能のキーワード: kinase p110, p110-gamma, lipid kinase, cytoplasmic, transferase-transferase inhibitor complex, transferase/transferase inhibitor
• 由来する生物種: Homo sapiens (human)
• 細胞内の位置: Cytoplasm: P48736
• タンパク質・核酸の鎖数: 1
• 化学式量合計: 111186.62

構造登録者

Murray, J.M. (登録日: 2012-05-02, 公開日: 2013-04-17, 最終更新日: 2023-09-13)

• 主引用文献: Sutherlin, D.P.,Baker, S.,Bisconte, A.,Blaney, P.M.,Brown, A.,Chan, B.K.,Chantry, D.,Castanedo, G.,DePledge, P.,Goldsmith, P.,Goldstein, D.M.,Hancox, T.,Kaur, J.,Knowles, D.,Kondru, R.,Lesnick, J.,Lucas, M.C.,Lewis, C.,Murray, J.,Nadin, A.J.,Nonomiya, J.,Pang, J.,Pegg, N.,Price, S.,Reif, K.,Safina, B.S.,Salphati, L.,Staben, S.,Seward, E.M.,Shuttleworth, S.,Sohal, S.,Sweeney, Z.K.,Ultsch, M.,Waszkowycz, B.,Wei, B.; Potent and selective inhibitors of PI3K-delta: obtaining isoform selectivity from the affinity pocket and tryptophan shelf; Bioorg.Med.Chem.Lett., 22:4296-4302, 2012; PubMed: 22672799; DOI: 10.1016/j.bmcl.2012.05.027

実験手法

X-RAY DIFFRACTION (2.803 Å)