8CSG

Human PRMT5:MEP50 structure with Fragment 1 and MTA Bound

Summary for 8CSG

• Entry DOI: 10.2210/pdb8csg/pdb
• Descriptor: Protein arginine N-methyltransferase 5, Methylosome protein 50, 6-bromo-1H-pyrrolo[3,2-b]pyridin-5-amine, ... (7 entities in total)
• Functional Keywords: mtap, methyl transferase, fragment-based lead discovery, fbdd, transferase
• Biological source: Homo sapiens (human); More
• Total number of polymer chains: 2
• Total formula weight: 112577.91

Authors

Gunn, R.J.,Lawson, J.D.,Smith, C.R. (deposition date: 2022-05-12, release date: 2022-10-05, Last modification date: 2023-01-11)

• Primary citation: Smith, C.R.,Kulyk, S.,Ahmad, M.U.D.,Arkhipova, V.,Christensen, J.G.,Gunn, R.J.,Ivetac, A.,Ketcham, J.M.,Kuehler, J.,Lawson, J.D.,Thomas, N.C.,Wang, X.,Marx, M.A.; Fragment optimization and elaboration strategies - the discovery of two lead series of PRMT5/MTA inhibitors from five fragment hits.; Rsc Med Chem, 13:1549-1564, 2022; PubMed: 36545438; DOI: 10.1039/d2md00163b

Experimental method

X-RAY DIFFRACTION (2.48 Å)