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PDBsum entry 5lvq
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PDB id:
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Transferase
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Title:
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Crystal structure of human pcaf bromodomain in complex with compound-d (cpd-d), n-methyl-2-(tetrahydro-2h-pyran-4-yloxy)benzamide
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Structure:
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Histone acetyltransferase kat2b. Chain: a, b. Synonym: histone acetyltransferase pcaf,histone acetylase pcaf,lysine acetyltransferase 2b,p300/cbp-associated factor,p/caf. Engineered: yes
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Source:
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Homo sapiens. Human. Organism_taxid: 9606. Gene: kat2b, pcaf. Expressed in: escherichia coli. Expression_system_taxid: 469008. Expression_system_variant: r3-prare2.
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Resolution:
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2.05Å
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R-factor:
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0.182
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R-free:
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0.218
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Authors:
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A.Chaikuad,P.Filippakopoulos,F.Von Delft,C.Bountra,C.H.Arrowsmith, A.M.Edwards,A.L.Hopkins,S.Knapp,Structural Genomics Consortium (Sgc)
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Key ref:
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I.Navratilova
et al.
(2016).
Discovery of New Bromodomain Scaffolds by Biosensor Fragment Screening.
Acs Med Chem Lett,
7,
1213-1218.
PubMed id:
DOI:
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Date:
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14-Sep-16
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Release date:
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26-Oct-16
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PROCHECK
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Headers
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References
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Q92831
(KAT2B_HUMAN) -
Histone acetyltransferase KAT2B from Homo sapiens
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Seq:
Struc:
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832 a.a.
108 a.a.
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Key: |
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PfamA domain |
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Secondary structure |
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CATH domain |
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Enzyme class 1:
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E.C.2.3.1.48
- histone acetyltransferase.
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Reaction:
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L-lysyl-[protein] + acetyl-CoA = N6-acetyl-L-lysyl-[protein] + CoA + H+
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L-lysyl-[protein]
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+
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acetyl-CoA
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=
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N(6)-acetyl-L-lysyl-[protein]
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+
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CoA
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+
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H(+)
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Enzyme class 2:
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E.C.2.3.1.57
- diamine N-acetyltransferase.
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Reaction:
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an alkane-alpha,omega-diamine + acetyl-CoA = an N-acetylalkane- alpha,omega-diamine + CoA + H+
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alkane-alpha,omega-diamine
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+
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acetyl-CoA
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=
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N-acetylalkane- alpha,omega-diamine
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+
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CoA
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+
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H(+)
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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 Med Chem Lett
7:1213-1218
(2016)
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PubMed id:
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Discovery of New Bromodomain Scaffolds by Biosensor Fragment Screening.
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I.Navratilova,
T.Aristotelous,
S.Picaud,
A.Chaikuad,
S.Knapp,
P.Filappakopoulos,
A.L.Hopkins.
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ABSTRACT
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