5U8A

Polycomb protein EED in complex with inhibitor: (3R,4S)-1-[(2-bromo-6-fluorophenyl)methyl]-N,N-dimethyl-4-(1-methyl-1H-indol-3-yl)pyrrolidin-3-amine

Summary for 5U8A

• Entry DOI: 10.2210/pdb5u8a/pdb
• Related: 5u8f
• Descriptor: Polycomb protein EED, (3R,4S)-1-[(2-bromo-6-fluorophenyl)methyl]-N,N-dimethyl-4-(1-methyl-1H-indol-3-yl)pyrrolidin-3-amine (3 entities in total)
• Functional Keywords: wd40 prc2, protein binding-inhibitor complex, protein binding/inhibitor
• Biological source: Homo sapiens (Human)
• Cellular location: Nucleus: O75530
• Total number of polymer chains: 1
• Total formula weight: 43013.84

Authors

Jakob, C.G.,Zhu, H. (deposition date: 2016-12-14, release date: 2017-03-15, Last modification date: 2023-10-04)

• Primary citation: Curtin, M.L.,Pliushchev, M.A.,Li, H.Q.,Torrent, M.,Dietrich, J.D.,Jakob, C.G.,Zhu, H.,Zhao, H.,Wang, Y.,Ji, Z.,Clark, R.F.,Sarris, K.A.,Selvaraju, S.,Shaw, B.,Algire, M.A.,He, Y.,Richardson, P.L.,Sweis, R.F.,Sun, C.,Chiang, G.G.,Michaelides, M.R.; SAR of amino pyrrolidines as potent and novel protein-protein interaction inhibitors of the PRC2 complex through EED binding.; Bioorg. Med. Chem. Lett., 27:1576-1583, 2017; PubMed: 28254486; DOI: 10.1016/j.bmcl.2017.02.030

Experimental method

X-RAY DIFFRACTION (1.45 Å)