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PDBsum entry 5ktw
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PDB id:
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Transferase
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Title:
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Crebbp bromodomain in complex with cpd 44 (3-((5-acetyl-1- (cyclopropylmethyl)-4,5,6,7-tetrahydro-1h-pyrazolo[4,3-c]pyridin-3- yl)amino)-n-isopropylbenzamide)
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Structure:
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Creb-binding protein. Chain: a, b, c. Fragment: bromodomain (unp residues 1085-1196). Engineered: yes
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Source:
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Homo sapiens. Human. Organism_taxid: 9606. Gene: crebbp, cbp. Expressed in: escherichia coli. Expression_system_taxid: 562.
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Resolution:
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1.09Å
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R-factor:
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0.163
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R-free:
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0.176
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Authors:
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J.M.Murray,G.Boenig
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Key ref:
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T.D.Crawford
et al.
(2016).
Discovery of a Potent and Selective in Vivo Probe (GNE-272) for the Bromodomains of CBP/EP300.
J Med Chem,
59,
10549-10563.
PubMed id:
DOI:
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Date:
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12-Jul-16
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Release date:
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02-Nov-16
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PROCHECK
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Headers
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References
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Q92793
(CBP_HUMAN) -
CREB-binding protein from Homo sapiens
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Seq:
Struc:
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2442 a.a.
114 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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*
PDB and UniProt seqs differ
at 3 residue positions (black
crosses)
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Enzyme class 1:
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E.C.2.3.1.-
- ?????
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Enzyme class 2:
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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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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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J Med Chem
59:10549-10563
(2016)
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PubMed id:
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Discovery of a Potent and Selective in Vivo Probe (GNE-272) for the Bromodomains of CBP/EP300.
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T.D.Crawford,
F.A.Romero,
K.W.Lai,
V.Tsui,
A.M.Taylor,
G.de Leon Boenig,
C.L.Noland,
J.Murray,
J.Ly,
E.F.Choo,
T.L.Hunsaker,
E.W.Chan,
M.Merchant,
S.Kharbanda,
K.E.Gascoigne,
S.Kaufman,
M.H.Beresini,
J.Liao,
W.Liu,
K.X.Chen,
Z.Chen,
A.R.Conery,
A.Côté,
H.Jayaram,
Y.Jiang,
J.R.Kiefer,
T.Kleinheinz,
Y.Li,
J.Maher,
E.Pardo,
F.Poy,
K.L.Spillane,
F.Wang,
J.Wang,
X.Wei,
Z.Xu,
Z.Xu,
I.Yen,
L.Zawadzke,
X.Zhu,
S.Bellon,
R.Cummings,
A.G.Cochran,
B.K.Albrecht,
S.Magnuson.
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ABSTRACT
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Links
