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PDBsum entry 5lsy
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PDB id:
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Transferase
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Title:
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Structure of the epigenetic oncogene mmset and inhibition by n-alkyl sinefungin derivatives
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Structure:
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Histone-lysine n-methyltransferase setd2. Chain: a. Fragment: unp residues 1433-1711. Synonym: hif-1,huntingtin yeast partner b,huntingtin-interacting protein 1,hip-1,huntingtin-interacting protein b,lysine n- methyltransferase 3a,set domain-containing protein 2,hset2,p231hbp. Engineered: yes
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Source:
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Homo sapiens. Human. Organism_taxid: 9606. Gene: setd2, hif1, hypb, kiaa1732, kmt3a, set2, hspc069. Expressed in: escherichia coli bl21(de3). Expression_system_taxid: 469008. Expression_system_variant: codon plus ril
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Resolution:
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1.62Å
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R-factor:
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0.183
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R-free:
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0.215
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Authors:
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D.Tisi,P.Pathuri,T.Heightman
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Key ref:
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D.Tisi
et al.
(2016).
Structure of the Epigenetic Oncogene MMSET and Inhibition by N-Alkyl Sinefungin Derivatives.
Acs Chem Biol,
11,
3093-3105.
PubMed id:
DOI:
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Date:
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05-Sep-16
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Release date:
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12-Oct-16
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PROCHECK
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Headers
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References
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Q9BYW2
(SETD2_HUMAN) -
Histone-lysine N-methyltransferase SETD2 from Homo sapiens
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Seq:
Struc:
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2564 a.a.
246 a.a.
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Key: |
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PfamA domain |
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Secondary structure |
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Enzyme class 2:
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E.C.2.1.1.-
- ?????
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Enzyme class 3:
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E.C.2.1.1.359
- [histone H3]-lysine(36) N-trimethyltransferase.
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Reaction:
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L-lysyl36-[histone H3] + 3 S-adenosyl-L-methionine = N6,N6,N6- trimethyl-L-lysyl36-[histone H3] + 3 S-adenosyl-L-homocysteine + 3 H+
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L-lysyl(36)-[histone H3]
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+
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3
×
S-adenosyl-L-methionine
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=
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N(6),N(6),N(6)- trimethyl-L-lysyl(36)-[histone H3]
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+
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3
×
S-adenosyl-L-homocysteine
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+
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3
×
H(+)
Bound ligand (Het Group name = )
matches with 46.15% similarity
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Note, where more than one E.C. class is given (as above), each may
correspond to a different protein domain or, in the case of polyprotein
precursors, to a different mature protein.
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Molecule diagrams generated from .mol files obtained from the
KEGG ftp site
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DOI no:
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Acs Chem Biol
11:3093-3105
(2016)
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PubMed id:
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Structure of the Epigenetic Oncogene MMSET and Inhibition by N-Alkyl Sinefungin Derivatives.
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D.Tisi,
E.Chiarparin,
E.Tamanini,
P.Pathuri,
J.E.Coyle,
A.Hold,
F.P.Holding,
N.Amin,
A.C.Martin,
S.J.Rich,
V.Berdini,
J.Yon,
P.Acklam,
R.Burke,
L.Drouin,
J.E.Harmer,
F.Jeganathan,
R.L.van Montfort,
Y.Newbatt,
M.Tortorici,
M.Westlake,
A.Wood,
S.Hoelder,
T.D.Heightman.
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ABSTRACT
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Links
