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PDBsum entry 5a83
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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-Based optimization of naphthyridones into potent atad2 bromodomain inhibitors.
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Authors
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P.Bamborough,
C.W.Chung,
R.C.Furze,
P.Grandi,
A.M.Michon,
R.J.Sheppard,
H.Barnett,
H.Diallo,
D.P.Dixon,
C.Douault,
E.J.Jones,
B.Karamshi,
D.J.Mitchell,
R.K.Prinjha,
C.Rau,
R.J.Watson,
T.Werner,
E.H.Demont.
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Ref.
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J Med Chem, 2015,
58,
6151-6178.
[DOI no: ]
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PubMed id
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Abstract
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ATAD2 is a bromodomain-containing protein whose overexpression is linked to poor
outcomes in a number of different cancer types. To date, no potent and selective
inhibitors of the bromodomain have been reported. This article describes the
structure-based optimization of a series of naphthyridones from micromolar leads
with no selectivity over the BET bromodomains to inhibitors with sub-100 nM
ATAD2 potency and 100-fold BET selectivity.
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