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PDBsum entry 4xub
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Transcription
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PDB id
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4xub
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References listed in PDB file
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Key reference
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Title
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Structure enabled design of baz2-Icr, A chemical probe targeting the bromodomains of baz2a and baz2b.
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Authors
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L.Drouin,
S.Mcgrath,
L.R.Vidler,
A.Chaikuad,
O.Monteiro,
C.Tallant,
M.Philpott,
C.Rogers,
O.Fedorov,
M.Liu,
W.Akhtar,
A.Hayes,
F.Raynaud,
S.Müller,
S.Knapp,
S.Hoelder.
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Ref.
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J Med Chem, 2015,
58,
2553-2559.
[DOI no: ]
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PubMed id
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Abstract
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The bromodomain containing proteins BAZ2A/B play essential roles in chromatin
remodeling and regulation of noncoding RNAs. We present the structure based
discovery of a potent, selective, and cell active inhibitor 13 (BAZ2-ICR) of the
BAZ2A/B bromodomains through rapid optimization of a weakly potent starting
point. A key feature of the presented inhibitors is an intramolecular aromatic
stacking interaction that efficiently occupies the shallow bromodomain pockets.
13 represents an excellent chemical probe for functional studies of the BAZ2
bromodomains in vitro and in vivo.
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