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PDBsum entry 4nra
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Transcription
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PDB id
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4nra
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References listed in PDB file
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Key reference
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Title
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Targeting low-Druggability bromodomains: fragment based screening and inhibitor design against the baz2b bromodomain.
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Authors
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F.M.Ferguson,
O.Fedorov,
A.Chaikuad,
M.Philpott,
J.R.Muniz,
I.Felletar,
F.Von delft,
T.Heightman,
S.Knapp,
C.Abell,
A.Ciulli.
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Ref.
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J Med Chem, 2013,
56,
10183-10187.
[DOI no: ]
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PubMed id
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Abstract
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Bromodomains are epigenetic reader domains that have recently become popular
targets. In contrast to BET bromodomains, which have proven druggable,
bromodomains from other regions of the phylogenetic tree have shallower pockets.
We describe successful targeting of the challenging BAZ2B bromodomain using
biophysical fragment screening and structure-based optimization of high
ligand-efficiency fragments into a novel series of low-micromolar inhibitors.
Our results provide attractive leads for development of BAZ2B chemical probes
and indicate the whole family may be tractable.
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