3L16

Discovery of (thienopyrimidin-2-yl)aminopyrimidines as Potent, Selective, and Orally Available Pan-PI3-Kinase and Dual Pan-PI3-Kinase/mTOR Inhibitors for the Treatment of Cancer

3L16 の概要

• エントリーDOI: 10.2210/pdb3l16/pdb
• 関連するPDBエントリー: 3L13 3L17
• 分子名称: Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma isoform, 5-(6-{[4-(methylsulfonyl)piperazin-1-yl]methyl}-4-morpholin-4-ylthieno[3,2-d]pyrimidin-2-yl)pyridin-2-amine (2 entities in total)
• 機能のキーワード: kinase, atp-binding, nucleotide-binding, transferase, pi3k-gamma p110 gamma
• 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: 111216.72

構造登録者

Murray, J.M.,Wiesmann, C. (登録日: 2009-12-10, 公開日: 2010-02-16, 最終更新日: 2023-09-06)

• 主引用文献: Sutherlin, D.P.,Sampath, D.,Berry, M.,Castanedo, G.,Chang, Z.,Chuckowree, I.,Dotson, J.,Folkes, A.,Friedman, L.,Goldsmith, R.,Heffron, T.,Lee, L.,Lesnick, J.,Lewis, C.,Mathieu, S.,Nonomiya, J.,Olivero, A.,Pang, J.,Prior, W.W.,Salphati, L.,Sideris, S.,Tian, Q.,Tsui, V.,Wan, N.C.,Wang, S.,Wiesmann, C.,Wong, S.,Zhu, B.Y.; Discovery of (Thienopyrimidin-2-yl)aminopyrimidines as Potent, Selective, and Orally Available Pan-PI3-Kinase and Dual Pan-PI3-Kinase/mTOR Inhibitors for the Treatment of Cancer.; J.Med.Chem., 53:1086-1097, 2010; PubMed: 20050669; DOI: 10.1021/jm901284w

実験手法

X-RAY DIFFRACTION (2.9 Å)