5LSX

Structure of the Epigenetic Oncogene MMSET and inhibition by N-Alkyl Sinefungin Derivatives

Summary for 5LSX

• Entry DOI: 10.2210/pdb5lsx/pdb
• Descriptor: Histone-lysine N-methyltransferase SETD2, ZINC ION, [(2~{R},5~{S})-1-[(2~{R},3~{S},4~{R},5~{R})-5-(6-aminopurin-9-yl)-3,4-bis(oxidanyl)oxolan-2-yl]-5-azaniumyl-6-oxidanyl-6-oxidanylidene-hexan-2-yl]-(phenylmethyl)azanium, ... (4 entities in total)
• Functional Keywords: lysine methyltransferase setd2 set domain, setd2#1, transferase
• Biological source: Homo sapiens (Human)
• Total number of polymer chains: 1
• Total formula weight: 34768.56

Authors

Tisi, D.,Pathuri, P.,Heightman, T. (deposition date: 2016-09-05, release date: 2016-10-05, Last modification date: 2024-05-08)

• Primary citation: Tisi, D.,Chiarparin, E.,Tamanini, E.,Pathuri, P.,Coyle, J.E.,Hold, A.,Holding, F.P.,Amin, N.,Martin, A.C.,Rich, S.J.,Berdini, V.,Yon, J.,Acklam, P.,Burke, R.,Drouin, L.,Harmer, J.E.,Jeganathan, F.,van Montfort, R.L.,Newbatt, Y.,Tortorici, M.,Westlake, M.,Wood, A.,Hoelder, S.,Heightman, T.D.; Structure of the Epigenetic Oncogene MMSET and Inhibition by N-Alkyl Sinefungin Derivatives.; ACS Chem. Biol., 11:3093-3105, 2016; PubMed: 27571355; DOI: 10.1021/acschembio.6b00308

Experimental method

X-RAY DIFFRACTION (2.9 Å)