7S1Q
PRMT5/MEP50 crystal structure with MTA and a phthalazinone inhibitor bound (Compound 9)
Summary for 7S1Q
Entry DOI | 10.2210/pdb7s1q/pdb |
Related | 7S0U 7S1P 7S1R 7S1S 7SER 7SES |
Descriptor | Protein arginine N-methyltransferase 5, Methylosome protein 50, 5'-DEOXY-5'-METHYLTHIOADENOSINE, ... (5 entities in total) |
Functional Keywords | prmt5, mtap, mta, methyl transferase, collateral lethality, synthetic lethality, fragment-based lead discovery, transferase, transferase-inhibitor complex, transferase/inhibitor |
Biological source | Homo sapiens (Human) More |
Total number of polymer chains | 2 |
Total formula weight | 112179.65 |
Authors | Gunn, R.J.,Thomas, N.C.,Lawson, J.D.,Ivetac, A.,Smith, C.R.,Kulyk, S.,Marx, M.A. (deposition date: 2021-09-02, 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 Cited by PubMed: 35041419DOI: 10.1021/acs.jmedchem.1c01900 PDB entries with the same primary citation |
Experimental method | X-RAY DIFFRACTION (2.78 Å) |
Structure validation
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