5K0M

Targeting the PRC2 complex through a novel protein-protein interaction inhibitor of EED

Summary for 5K0M

• Entry DOI: 10.2210/pdb5k0m/pdb
• Descriptor: Polycomb protein EED, (3R,4S)-1-[(1S)-7-fluoro-2,3-dihydro-1H-inden-1-yl]-N,N-dimethyl-4-{4-[4-(methylsulfonyl)piperazin-1-yl]phenyl}pyrrolidin-3-amine (3 entities in total)
• Functional Keywords: wd40 prc2, protein binding
• Biological source: Homo sapiens (Human)
• Cellular location: Nucleus: O75530
• Total number of polymer chains: 1
• Total formula weight: 43423.57

Authors

Jakob, C.G.,Bigelow, L.J.,Zhu, H.,Sun, C. (deposition date: 2016-05-17, release date: 2017-01-25, Last modification date: 2023-09-27)

• Primary citation: He, Y.,Selvaraju, S.,Curtin, M.L.,Jakob, C.G.,Zhu, H.,Comess, K.M.,Shaw, B.,The, J.,Lima-Fernandes, E.,Szewczyk, M.M.,Cheng, D.,Klinge, K.L.,Li, H.Q.,Pliushchev, M.,Algire, M.A.,Maag, D.,Guo, J.,Dietrich, J.,Panchal, S.C.,Petros, A.M.,Sweis, R.F.,Torrent, M.,Bigelow, L.J.,Senisterra, G.,Li, F.,Kennedy, S.,Wu, Q.,Osterling, D.J.,Lindley, D.J.,Gao, W.,Galasinski, S.,Barsyte-Lovejoy, D.,Vedadi, M.,Buchanan, F.G.,Arrowsmith, C.H.,Chiang, G.G.,Sun, C.,Pappano, W.N.; The EED protein-protein interaction inhibitor A-395 inactivates the PRC2 complex.; Nat. Chem. Biol., 13:389-395, 2017; PubMed: 28135237; DOI: 10.1038/nchembio.2306

Experimental method

X-RAY DIFFRACTION (1.83 Å)