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TitleAnti-tumor Activity of the Type I PRMT Inhibitor, GSK3368715, Synergizes with PRMT5 Inhibition through MTAP Loss.
Journal, issue, pagesCancer Cell, Vol. 36, Page 100-, Year 2019
Publish dateJan 28, 2019 (structure data deposition date)
AuthorsFedoriw, 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. ...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.
External linksCancer Cell / PubMed:31257072
MethodsX-ray diffraction
Resolution2.48 Å
Structure data

PDB-6nt2:
type 1 PRMT in complex with the inhibitor GSK3368715
Method: X-RAY DIFFRACTION / Resolution: 2.48 Å

Chemicals

ChemComp-SAH:
S-ADENOSYL-L-HOMOCYSTEINE

ChemComp-KZS:
N~1~-({5-[4,4-bis(ethoxymethyl)cyclohexyl]-1H-pyrazol-4-yl}methyl)-N~1~,N~2~-dimethylethane-1,2-diamine

ChemComp-GOL:
GLYCEROL

ChemComp-DTT:
2,3-DIHYDROXY-1,4-DITHIOBUTANE

ChemComp-HOH:
WATER

Source
  • homo sapiens (human)
KeywordsANTITUMOR PROTEIN / inhibitor / cmplex / methyl transferase / arginine

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