4QL1

Crystal structure of human WDR5 in complex with compound OICR-9429

Summary for 4QL1

• Entry DOI: 10.2210/pdb4ql1/pdb
• Descriptor: WD repeat-containing protein 5, N-(4-(4-methylpiperazin-1-yl)-3'-(morpholinomethyl)-[1,1'-biphenyl]-3-yl)-6-oxo-4-(trifluoromethyl)-1,6-dihydropyridine-3-carboxamide, UNKNOWN ATOM OR ION, ... (6 entities in total)
• Functional Keywords: wdr5, wd repeat domain 5, oicr-9429 inhibitor, structural genomics, structural genomics consortium, sgc, transcription-inhibitor complex, transcription/inhibitor
• Biological source: Homo sapiens (human)
• Cellular location: Nucleus : P61964
• Total number of polymer chains: 2
• Total formula weight: 69845.12

Authors

Dong, A.,Dombrovski, L.,Walker, J.R.,Getlik, M.,Kuznetsova, E.,Smil, D.,Barsyte, D.,Li, F.,Poda, G.,Senisterra, G.,Marcellus, R.,Al-Awar, R.,Bountra, C.,Arrowsmith, C.H.,Edwards, A.M.,Brown, P.J.,Schapira, M.,Vedadi, M.,Wu, H.,Structural Genomics Consortium (SGC) (deposition date: 2014-06-10, release date: 2014-12-17, Last modification date: 2023-09-20)

• Primary citation: Grebien, F.,Vedadi, M.,Getlik, M.,Giambruno, R.,Grover, A.,Avellino, R.,Skucha, A.,Vittori, S.,Kuznetsova, E.,Smil, D.,Barsyte-Lovejoy, D.,Li, F.,Poda, G.,Schapira, M.,Wu, H.,Dong, A.,Senisterra, G.,Stukalov, A.,Huber, K.V.,Schonegger, A.,Marcellus, R.,Bilban, M.,Bock, C.,Brown, P.J.,Zuber, J.,Bennett, K.L.,Al-Awar, R.,Delwel, R.,Nerlov, C.,Arrowsmith, C.H.,Superti-Furga, G.; Pharmacological targeting of the Wdr5-MLL interaction in C/EBP alpha N-terminal leukemia.; Nat.Chem.Biol., 11:571-578, 2015; PubMed: 26167872; DOI: 10.1038/nchembio.1859

Experimental method

X-RAY DIFFRACTION (1.5 Å)