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Ligands
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C7N 2-(1-methylpiperidin-4-ylidene)tricyclo[9.4.0.0^{3,8}]pentadeca-1(11),3(8),4,6,9,12,14-heptaen-6-ol
GOL Glycerol
SFG Sinefungin
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Code : 5YLT   PDBj   RCSB PDB   PDBe
Header : TRANSFERASE/TRANSFERASE INHIBITOR
Title : Crystal structure of SET7/9 in complex with a cyproheptadine derivative
Release Data : 2018-06-20
Compound :
mol_id molecule chains synonym
1 Histone-lysine N-methyltransferase SETD7 A Histone H3-K4 methyltransferase SETD7,H3-K4-HMTase SETD7,Lysine N-methyltransferase 7,SET domain-containing protein 7,SET7/9
ec: 2.1.1.43
Source :
mol_id organism_scientific organism_common expression_system
1 Homo sapiens  (taxid:9606) Human CELL-FREE SYNTHESIS  (taxid:32644)
gene: SETD7, KIAA1717, KMT7, SET7, SET9
expression_system_vector_type: PLASMID
expression_system_plasmid: PX100709-08
Authors : Hirano, T., Fujiwara, T., Niwa, H., Hirano, M., Ohira, K., Okazaki, Y., Sato, S., Umehara, T., Maemoto, Y., Ito, A., Yoshida, M., Kagechika, H.
Keywords : Set domain, methyltransferase, inhibitor, TRANSFERASE, TRANSFERASE-TRANSFERASE INHIBITOR complex
Exp. method : X-RAY DIFFRACTION ( 1.690 Å )
Citation :

Development of Novel Inhibitors for Histone Methyltransferase SET7/9 based on Cyproheptadine.

Hirano, T.,Fujiwara, T.,Niwa, H.  et al.
(2018)  ChemMedChem  13 : 1530 - 1540

PubMed: 29882380
DOI: 10.1002/cmdc.201800233

Chain : A
UniProt : Q8WTS6 (SETD7_HUMAN)
Reaction: EC: Evidence:
Physiological Direction:
L-lysyl(4)-[histone H3] + S-adenosyl-L-methionine = H(+) + N(6)-methyl-L-lysyl(4)-[histone H3] + S-adenosyl-L-homocysteine 2.1.1.364 PROSITE-ProRule:PRU00910, PubMed:12540855
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L-lysyl-[protein] + S-adenosyl-L-methionine = H(+) + N(6)- methyl-L-lysyl-[protein] + S-adenosyl-L-homocysteine - PubMed:15099517, PubMed:15525938, PubMed:16415881
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