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PDBsum entry 5a5p
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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 low-Micromolar atad2 bromodomain inhibitors.
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Authors
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E.H.Demont,
C.W.Chung,
R.C.Furze,
P.Grandi,
A.M.Michon,
C.Wellaway,
N.Barrett,
A.M.Bridges,
P.D.Craggs,
H.Diallo,
D.P.Dixon,
C.Douault,
A.J.Emmons,
E.J.Jones,
B.V.Karamshi,
K.Locke,
D.J.Mitchell,
B.H.Mouzon,
R.K.Prinjha,
A.D.Roberts,
R.J.Sheppard,
R.J.Watson,
P.Bamborough.
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Ref.
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J Med Chem, 2015,
58,
5649-5673.
[DOI no: ]
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PubMed id
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Abstract
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Overexpression of ATAD2 (ATPase family, AAA domain containing 2) has been linked
to disease severity and progression in a wide range of cancers, and is
implicated in the regulation of several drivers of cancer growth. Little is
known of the dependence of these effects upon the ATAD2 bromodomain, which has
been categorized as among the least tractable of its class. The absence of any
potent, selective inhibitors limits clear understanding of the therapeutic
potential of the bromodomain. Here, we describe the discovery of a hit from a
fragment-based targeted array. Optimization of this produced the first known
micromolar inhibitors of the ATAD2 bromodomain.
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