3RKZ

Discovery of a stable macrocyclic o-aminobenzamide Hsp90 inhibitor capable of significantly decreasing tumor volume in a mouse xenograft model.

3RKZ の概要

• エントリーDOI: 10.2210/pdb3rkz/pdb
• 分子名称: Heat shock protein HSP 90-alpha, (5R,6S)-3-(L-alanyl)-5,6,15,15,18-pentamethyl-17-oxo-2,3,4,5,6,7,14,15,16,17-decahydro-1H-12,8-(metheno)[1,5,9]triazacyclotetradecino[1,2-a]indole-9-carboxamide (3 entities in total)
• 機能のキーワード: chaperone, atp binding domain, atp-binding, nucleotide-binding, phosphoprotein, stress response, chaperone-chaperone inhibitor complex, chaperone/chaperone inhibitor
• 由来する生物種: Homo sapiens (human)
• 細胞内の位置: Cytoplasm: P07900
• タンパク質・核酸の鎖数: 1
• 化学式量合計: 25906.21

構造登録者

Zapf, C.W.,Bloom, J.D.,Li, Z.,Dushin, R.G.,Nittoli, T.,Otteng, M.,Nikitenko, A.,Golas, J.M.,Liu, H.,Lucas, J.,Boschelli, F.,Vogan, E.,Olland, A.,Johnson, M.,Levin, J.I. (登録日: 2011-04-18, 公開日: 2011-07-13, 最終更新日: 2023-09-13)

• 主引用文献: Zapf, C.W.,Bloom, J.D.,Li, Z.,Dushin, R.G.,Nittoli, T.,Otteng, M.,Nikitenko, A.,Golas, J.M.,Liu, H.,Lucas, J.,Boschelli, F.,Vogan, E.,Olland, A.,Johnson, M.,Levin, J.I.; Discovery of a stable macrocyclic o-aminobenzamide Hsp90 inhibitor which significantly decreases tumor volume in a mouse xenograft model.; Bioorg.Med.Chem.Lett., 21:4602-4607, 2011; PubMed: 21715165; DOI: 10.1016/j.bmcl.2011.05.102

実験手法

X-RAY DIFFRACTION (1.5693 Å)