7M05

CryoEM structure of PRMT5 bound to covalent PBM-site inhibitor BRD-6988

7M05 の概要

• エントリーDOI: 10.2210/pdb7m05/pdb
• EMDBエントリー: 23609
• 分子名称: Protein arginine N-methyltransferase 5, Methylosome protein 50, 2-(5-chloro-6-oxopyridazin-1(6H)-yl)-N-(4-methyl-3-{[2-(pyridin-2-yl)ethyl]sulfamoyl}phenyl)acetamide (3 entities in total)
• 機能のキーワード: methyltransferase, splicing, epigenetic, transferase-inhibitor complex, transferase/inhibitor
• 由来する生物種: Homo sapiens (Human); 詳細
• タンパク質・核酸の鎖数: 8
• 化学式量合計: 439807.00

構造登録者

McMillan, B.J.,McKinney, D.C.,Timm, D.E. (登録日: 2021-03-10, 公開日: 2021-03-17, 最終更新日: 2021-08-25)

• 主引用文献: McKinney, D.C.,McMillan, B.J.,Ranaghan, M.J.,Moroco, J.A.,Brousseau, M.,Mullin-Bernstein, Z.,O'Keefe, M.,McCarren, P.,Mesleh, M.F.,Mulvaney, K.M.,Robinson, F.,Singh, R.,Bajrami, B.,Wagner, F.F.,Hilgraf, R.,Drysdale, M.J.,Campbell, A.J.,Skepner, A.,Timm, D.E.,Porter, D.,Kaushik, V.K.,Sellers, W.R.,Ianari, A.; Discovery of a First-in-Class Inhibitor of the PRMT5-Substrate Adaptor Interaction.; J.Med.Chem., 64:11148-11168, 2021; PubMed: 34342224; DOI: 10.1021/acs.jmedchem.1c00507

実験手法

ELECTRON MICROSCOPY (2.39 Å)