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PDBsum entry 5i83
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Protein binding/inhibitor
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PDB id
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5i83
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References listed in PDB file
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Key reference
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Title
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Fragment-Based discovery of a selective and cell-Active benzodiazepinone cbp/ep300 bromodomain inhibitor (cpi-637).
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Authors
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A.M.Taylor,
A.Côté,
M.C.Hewitt,
R.Pastor,
Y.Leblanc,
C.G.Nasveschuk,
F.A.Romero,
T.D.Crawford,
N.Cantone,
H.Jayaram,
J.Setser,
J.Murray,
M.H.Beresini,
G.De leon boenig,
Z.Chen,
A.R.Conery,
R.T.Cummings,
L.A.Dakin,
E.M.Flynn,
O.W.Huang,
S.Kaufman,
P.J.Keller,
J.R.Kiefer,
T.Lai,
Y.Li,
J.Liao,
W.Liu,
H.Lu,
E.Pardo,
V.Tsui,
J.Wang,
Y.Wang,
Z.Xu,
F.Yan,
D.Yu,
L.Zawadzke,
X.Zhu,
X.Zhu,
R.J.Sims,
A.G.Cochran,
S.Bellon,
J.E.Audia,
S.Magnuson,
B.K.Albrecht.
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Ref.
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Acs Med Chem Lett, 2016,
7,
531-536.
[DOI no: ]
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PubMed id
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Abstract
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CBP and EP300 are highly homologous, bromodomain-containing transcription
coactivators involved in numerous cellular pathways relevant to oncology. As
part of our effort to explore the potential therapeutic implications of
selectively targeting bromodomains, we set out to identify a CBP/EP300
bromodomain inhibitor that was potent both in vitro and in cellular target
engagement assays and was selective over the other members of the bromodomain
family. Reported here is a series of cell-potent and selective probes of the
CBP/EP300 bromodomains, derived from the fragment screening hit
4-methyl-1,3,4,5-tetrahydro-2H-benzo[b][1,4]diazepin-2-one.
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