6NT2

type 1 PRMT in complex with the inhibitor GSK3368715

Summary for 6NT2

• Entry DOI: 10.2210/pdb6nt2/pdb
• Descriptor: Protein arginine N-methyltransferase 1, S-ADENOSYL-L-HOMOCYSTEINE, N~1~-({5-[4,4-bis(ethoxymethyl)cyclohexyl]-1H-pyrazol-4-yl}methyl)-N~1~,N~2~-dimethylethane-1,2-diamine, ... (6 entities in total)
• Functional Keywords: inhibitor, cmplex, methyl transferase, arginine, antitumor protein
• Biological source: Homo sapiens (Human)
• Total number of polymer chains: 4
• Total formula weight: 175322.42

Authors

Concha, N.O. (deposition date: 2019-01-28, release date: 2019-07-10, Last modification date: 2019-07-24)

• Primary citation: Fedoriw, A.,Rajapurkar, S.R.,O'Brien, S.,Gerhart, S.V.,Mitchell, L.H.,Adams, N.D.,Rioux, N.,Lingaraj, T.,Ribich, S.A.,Pappalardi, M.B.,Shah, N.,Laraio, J.,Liu, Y.,Butticello, M.,Carpenter, C.L.,Creasy, C.,Korenchuk, S.,McCabe, M.T.,McHugh, C.F.,Nagarajan, R.,Wagner, C.,Zappacosta, F.,Annan, R.,Concha, N.O.,Thomas, R.A.,Hart, T.K.,Smith, J.J.,Copeland, R.A.,Moyer, M.P.,Campbell, J.,Stickland, K.,Mills, J.,Jacques-O'Hagan, S.,Allain, C.,Johnston, D.,Raimondi, A.,Porter Scott, M.,Waters, N.,Swinger, K.,Boriack-Sjodin, A.,Riera, T.,Shapiro, G.,Chesworth, R.,Prinjha, R.K.,Kruger, R.G.,Barbash, O.,Mohammad, H.P.; Anti-tumor Activity of the Type I PRMT Inhibitor, GSK3368715, Synergizes with PRMT5 Inhibition through MTAP Loss.; Cancer Cell, 36:100-, 2019; PubMed: 31257072; DOI: 10.1016/j.ccell.2019.05.014

Experimental method

X-RAY DIFFRACTION (2.48 Å)