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PDBsum entry 5lpm
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Transcription
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PDB id
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5lpm
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References listed in PDB file
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Key reference
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Title
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Beyond the bet family: targeting cbp/p300 with 4-Acyl pyrroles.
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Authors
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M.Hügle,
X.Lucas,
D.Ostrovskyi,
P.Regenass,
S.Gerhardt,
O.Einsle,
M.Hau,
M.Jung,
B.Breit,
S.Günther,
D.Wohlwend.
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Ref.
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Angew Chem Int Ed Engl, 2017,
56,
12476-12480.
[DOI no: ]
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PubMed id
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Abstract
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Bromodomain and extra-terminal domain (BET) inhibitors are widely used both as
chemical tools to study the biological role of their targets in living organisms
and as candidates for drug development against several cancer variants and human
disorders. However, non-BET bromodomains such as those in p300 and CBP are less
studied. XDM-CBP is a highly potent and selective inhibitor for the bromodomains
of CBP and p300 derived from a pan-selective BET BRD-binding fragment. Along
with X-ray crystal-structure analysis and thermodynamic profiling, XDM-CBP was
used in screenings of several cancer cell lines in vitro to study its
inhibitory potential on cancer cell proliferation. XDM-CBP is demonstrated to be
a potent and selective CBP/p300 inhibitor that acts on specific cancer cell
lines, in particular malignant melanoma, breast cancer, and leukemia.
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