7MX7

PRMT5:MEP50 complexed with inhibitor PF-06939999

Summary for 7MX7

• Entry DOI: 10.2210/pdb7mx7/pdb
• Descriptor: Protein arginine N-methyltransferase 5, Methylosome protein 50, (1S,2S,3S,5R)-3-{[6-(difluoromethyl)-5-fluoro-1,2,3,4-tetrahydroisoquinolin-8-yl]oxy}-5-(4-methyl-7H-pyrrolo[2,3-d]pyrimidin-7-yl)cyclopentane-1,2-diol, ... (4 entities in total)
• Functional Keywords: arginine, methyl, transferase, transferase-transcription complex, transferase/transcription
• Biological source: Homo sapiens (Human); More
• Total number of polymer chains: 2
• Total formula weight: 112735.18

Authors

McTigue, M.,Deng, Y.L.,Liu, W.,Brooun, A. (deposition date: 2021-05-18, release date: 2021-11-17, Last modification date: 2023-10-18)

• Primary citation: Jensen-Pergakes, K.,Tatlock, J.,Maegley, K.A.,McAlpine, I.J.,McTigue, M.,Xie, T.,Dillon, C.P.,Wang, Y.,Yamazaki, S.,Spiegel, N.,Shi, M.,Nemeth, A.,Miller, N.,Hendrickson, E.,Lam, H.,Sherrill, J.,Chung, C.Y.,McMillan, E.A.,Bryant, S.K.,Palde, P.,Braganza, J.,Brooun, A.,Deng, Y.L.,Goshtasbi, V.,Kephart, S.E.,Kumpf, R.A.,Liu, W.,Patman, R.L.,Rui, E.,Scales, S.,Tran-Dube, M.,Wang, F.,Wythes, M.,Paul, T.A.; SAM-Competitive PRMT5 Inhibitor PF-06939999 Demonstrates Antitumor Activity in Splicing Dysregulated NSCLC with Decreased Liability of Drug Resistance.; Mol.Cancer Ther., 21:3-15, 2022; PubMed: 34737197; DOI: 10.1158/1535-7163.MCT-21-0620

Experimental method

X-RAY DIFFRACTION (2.49 Å)