7T7M

Structure of human GLP SET-domain (EHMT1) in complex with covalent inhibitor (Compound 1)

7T7M の概要

• エントリーDOI: 10.2210/pdb7t7m/pdb
• 分子名称: Histone-lysine N-methyltransferase EHMT1, ZINC ION, N-(6-methoxy-4-{[1-(propan-2-yl)piperidin-4-yl]amino}-7-[3-(pyrrolidin-1-yl)propoxy]quinazolin-2-yl)prop-2-enamide, ... (5 entities in total)
• 機能のキーワード: glp, covalent inhibitor, gene regulation, transferase-inhibitor complex, transferase/inhibitor
• 由来する生物種: Homo sapiens (human)
• タンパク質・核酸の鎖数: 4
• 化学式量合計: 134932.52

構造登録者

Park, K.-S.,Kumar, P. (登録日: 2021-12-15, 公開日: 2022-07-06, 最終更新日: 2023-10-18)

• 主引用文献: Park, K.S.,Xiong, Y.,Yim, H.,Velez, J.,Babault, N.,Kumar, P.,Liu, J.,Jin, J.; Discovery of the First-in-Class G9a/GLP Covalent Inhibitors.; J.Med.Chem., 65:10506-10522, 2022; PubMed: 35763668; DOI: 10.1021/acs.jmedchem.2c00652

実験手法

X-RAY DIFFRACTION (2.85 Å)