9EYW

Human PRMT5 in complex with AZ compound 21

This is a non-PDB format compatible entry.

Summary for 9EYW

• Entry DOI: 10.2210/pdb9eyw/pdb
• Descriptor: Protein arginine N-methyltransferase 5, N-terminally processed, Methylosome protein WDR77, (3~{S})-2-[(5-azanyl-1~{H}-pyrrolo[3,2-b]pyridin-2-yl)methyl]-6-fluoranyl-1'-[(4-fluorophenyl)methyl]spiro[isoindole-3,3'-pyrrolidine]-1,2'-dione, ... (6 entities in total)
• Functional Keywords: methyl transferase, inhibitor, transferase
• Biological source: Homo sapiens (human); More
• Total number of polymer chains: 2
• Total formula weight: 110390.78

Authors

Debreczeni, J. (deposition date: 2024-04-09, release date: 2024-08-14, Last modification date: 2024-09-04)

• Primary citation: Smith, J.M.,Barlaam, B.,Beattie, D.,Bradshaw, L.,Chan, H.M.,Chiarparin, E.,Collingwood, O.,Cooke, S.L.,Cronin, A.,Cumming, I.,Dean, E.,Debreczeni, J.E.,Del Barco Barrantes, I.,Diene, C.,Gianni, D.,Guerot, C.,Guo, X.,Guven, S.,Hayhow, T.G.,Hong, T.,Kemmitt, P.D.,Lamont, G.M.,Lamont, S.,Lynch, J.T.,McWilliams, L.,Moore, S.,Raubo, P.,Robb, G.R.,Robinson, J.,Scott, J.S.,Srinivasan, B.,Steward, O.,Stubbs, C.J.,Syson, K.,Tan, L.,Turner, O.,Underwood, E.,Urosevic, J.,Vazquez-Chantada, M.,Whittaker, A.L.,Wilson, D.M.,Winter-Holt, J.J.; Discovery and In Vivo Efficacy of AZ-PRMT5i-1, a Novel PRMT5 Inhibitor with High MTA Cooperativity.; J.Med.Chem., 67:13604-13638, 2024; PubMed: 39080842; DOI: 10.1021/acs.jmedchem.4c00097

Experimental method

X-RAY DIFFRACTION (2.3 Å)