7M05

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

Summary for 7M05

• Entry DOI: 10.2210/pdb7m05/pdb
• EMDB information: 23609
• Descriptor: 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)
• Functional Keywords: methyltransferase, splicing, epigenetic, transferase-inhibitor complex, transferase/inhibitor
• Biological source: Homo sapiens (Human); More
• Total number of polymer chains: 8
• Total formula weight: 439807.00

Authors

McMillan, B.J.,McKinney, D.C.,Timm, D.E. (deposition date: 2021-03-10, release date: 2021-03-17, Last modification date: 2021-08-25)

• Primary citation: 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

Experimental method

ELECTRON MICROSCOPY (2.39 Å)