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7KIB

PRMT5:MEP50 Complexed with 5,5-Bicyclic Inhibitor Compound 4

Summary for 7KIB
Entry DOI10.2210/pdb7kib/pdb
DescriptorProtein arginine N-methyltransferase 5, Methylosome protein 50, (2R,3R,3aS,6S,6aR)-6-[(2-amino-3-bromoquinolin-7-yl)oxy]-2-(4-amino-7H-pyrrolo[2,3-d]pyrimidin-7-yl)hexahydro-3aH-cyclopenta[b]furan-3,3a-diol, ... (7 entities in total)
Functional Keywordstransferase, transferase-transferase inhibitor complex, transferase/transferase inhibitor
Biological sourceHomo sapiens (Human)
More
Total number of polymer chains2
Total formula weight113078.65
Authors
Palte, R.L.,Hayes, R.P. (deposition date: 2020-10-23, release date: 2021-04-21, Last modification date: 2023-10-18)
Primary citationQuiroz, R.V.,Reutershan, M.H.,Schneider, S.E.,Sloman, D.,Lacey, B.M.,Swalm, B.M.,Yeung, C.S.,Gibeau, C.,Spellman, D.S.,Rankic, D.A.,Chen, D.,Witter, D.,Linn, D.,Munsell, E.,Feng, G.,Xu, H.,Hughes, J.M.E.,Lim, J.,Sauri, J.,Geddes, K.,Wan, M.,Mansueto, M.S.,Follmer, N.E.,Fier, P.S.,Siliphaivanh, P.,Daublain, P.,Palte, R.L.,Hayes, R.P.,Lee, S.,Kawamura, S.,Silverman, S.,Sanyal, S.,Henderson, T.J.,Ye, Y.,Gao, Y.,Nicholson, B.,Machacek, M.R.
The Discovery of Two Novel Classes of 5,5-Bicyclic Nucleoside-Derived PRMT5 Inhibitors for the Treatment of Cancer.
J.Med.Chem., 64:3911-3939, 2021
Cited by
PubMed: 33755451
DOI: 10.1021/acs.jmedchem.0c02083
PDB entries with the same primary citation
Experimental method
X-RAY DIFFRACTION (2.52 Å)
Structure validation

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