7S1S

PRMT5/MEP50 crystal structure with MTA and MRTX-1719 bound

7S1S の概要

• エントリーDOI: 10.2210/pdb7s1s/pdb
• 関連するPDBエントリー: 7S0U 7S1P 7S1Q 7S1R 7SER 7SES
• 分子名称: Protein arginine N-methyltransferase 5, Methylosome protein 50, 5'-DEOXY-5'-METHYLTHIOADENOSINE, ... (5 entities in total)
• 機能のキーワード: prmt5, mtap, mta, methyl transferase, collateral lethality, synthetic lethality, fragment-based lead discovery, transferase, 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: 2
• 化学式量合計: 112389.25

構造登録者

Gunn, R.J.,Thomas, N.C.,Lawson, J.D.,Ivetac, A.,Kulyk, S.,Smith, C.R.,Marx, M.A. (登録日: 2021-09-02, 公開日: 2022-01-26, 最終更新日: 2023-10-18)

• 主引用文献: Smith, C.R.,Aranda, R.,Bobinski, T.P.,Briere, D.M.,Burns, A.C.,Christensen, J.G.,Clarine, J.,Engstrom, L.D.,Gunn, R.J.,Ivetac, A.,Jean-Baptiste, R.,Ketcham, J.M.,Kobayashi, M.,Kuehler, J.,Kulyk, S.,Lawson, J.D.,Moya, K.,Olson, P.,Rahbaek, L.,Thomas, N.C.,Wang, X.,Waters, L.M.,Marx, M.A.; Fragment-Based Discovery of MRTX1719, a Synthetic Lethal Inhibitor of the PRMT5•MTA Complex for the Treatment of MTAP -Deleted Cancers.; J.Med.Chem., 65:1749-1766, 2022; PubMed: 35041419; DOI: 10.1021/acs.jmedchem.1c01900

実験手法

X-RAY DIFFRACTION (2.62 Å)