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PDBsum entry 5g4r
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Transcription
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PDB id
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5g4r
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PDB id:
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| Name: |
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Transcription
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Title:
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Bromodomain of human brpf1 with n-1,3-dimethyl-6-2r-2- methylpiperazin-1-yl-2-oxo-2,3-dihydro-1h-1,3-benzodiazol-5-yl-2- methoxybenzamide
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Structure:
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Peregrin. Chain: a, b, c, d. Fragment: bromodomain of brpf1, unp residues 622-738. Synonym: bromodomain and phd finger-containing protein 1, protein br140,. Engineered: yes
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Source:
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Homo sapiens. Human. Organism_taxid: 9606. Expressed in: escherichia coli. Expression_system_taxid: 562
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Resolution:
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1.96Å
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R-factor:
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0.202
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R-free:
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0.240
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Authors:
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C.Chung
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Key ref:
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P.Bamborough
et al.
(2016).
GSK6853, a Chemical Probe for Inhibition of the BRPF1 Bromodomain.
Acs Med Chem Lett,
7,
552-557.
PubMed id:
DOI:
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Date:
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16-May-16
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Release date:
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06-Jul-16
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PROCHECK
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Headers
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References
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P55201
(BRPF1_HUMAN) -
Peregrin from Homo sapiens
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Seq:
Struc:
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1214 a.a.
109 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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DOI no:
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Acs Med Chem Lett
7:552-557
(2016)
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PubMed id:
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GSK6853, a Chemical Probe for Inhibition of the BRPF1 Bromodomain.
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P.Bamborough,
H.A.Barnett,
I.Becher,
M.J.Bird,
C.W.Chung,
P.D.Craggs,
E.H.Demont,
H.Diallo,
D.J.Fallon,
L.J.Gordon,
P.Grandi,
C.I.Hobbs,
E.Hooper-Greenhill,
E.J.Jones,
R.P.Law,
A.Le Gall,
D.Lugo,
A.M.Michon,
D.J.Mitchell,
R.K.Prinjha,
R.J.Sheppard,
A.J.Watson,
R.J.Watson.
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ABSTRACT
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The BRPF (Bromodomain and PHD Finger-containing) protein family are important
scaffolding proteins for assembly of MYST histone acetyltransferase complexes. A
selective benzimidazolone BRPF1 inhibitor showing micromolar activity in a
cellular target engagement assay was recently described. Herein, we report the
optimization of this series leading to the identification of a superior BRPF1
inhibitor suitable for in vivo studies.
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Links
