7S0U

PRMT5/MEP50 crystal structure with MTA and phthalazinone fragment bound

Summary for 7S0U

• Entry DOI: 10.2210/pdb7s0u/pdb
• Related: 7S1P 7S1Q 7S1R 7S1S 7SER 7SES
• Descriptor: Protein arginine N-methyltransferase 5, Methylosome protein 50, CHLORIDE ION, ... (8 entities in total)
• Functional Keywords: prmt5, mtap, mta, methyl transferase, collateral lethality, synthetic lethality, fragment-based lead discovery, transferase
• Biological source: Homo sapiens (Human); More
• Total number of polymer chains: 2
• Total formula weight: 112219.06

Authors

Gunn, R.J.,Thomas, N.C.,Lawson, J.D.,Ivetac, A.,Smith, C.R.,Kulyk, S.,Marx, M.A. (deposition date: 2021-08-31, release date: 2022-01-26, Last modification date: 2023-10-18)

• Primary citation: 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

Experimental method

X-RAY DIFFRACTION (2.01 Å)