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PDBsum entry 6afb
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References listed in PDB file
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Key reference
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Title
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Discovery and optimization of inhibitors of the parkinson'S disease associated protein dj-1.
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Authors
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S.Tashiro,
J.M.M.Caaveiro,
M.Nakakido,
A.Tanabe,
S.Nagatoishi,
Y.Tamura,
N.Matsuda,
D.Liu,
Q.Q.Hoang,
K.Tsumoto.
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Ref.
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ACS Chem Biol, 2018,
13,
2783-2793.
[DOI no: ]
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PubMed id
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Abstract
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DJ-1 is a Parkinson's disease associated protein endowed with enzymatic, redox
sensing, regulatory, chaperoning, and neuroprotective activities. Although DJ-1
has been vigorously studied for the past decade and a half, its exact role in
the progression of the disease remains uncertain. In addition, little is known
about the spatiotemporal regulation of DJ-1, or the biochemical basis explaining
its numerous biological functions. Progress has been hampered by the lack of
inhibitors with precisely known mechanisms of action. Herein, we have employed
biophysical methodologies and X-ray crystallography to identify and to optimize
a family of compounds inactivating the critical Cys106 residue of human DJ-1. We
demonstrate these compounds are potent inhibitors of various activities of DJ-1
in vitro and in cell-based assays. This study reports a new family of DJ-1
inhibitors with a defined mechanism of action, and contributes toward the
understanding of the biological function of DJ-1.
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Secondary reference #1
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Title
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Thermodynamic and structural characterization of the specific binding of zn(ii) to human protein dj-1.
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Authors
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S.Tashiro,
J.M.Caaveiro,
C.X.Wu,
Q.Q.Hoang,
K.Tsumoto.
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Ref.
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Biochemistry, 2014,
53,
2218-2220.
[DOI no: ]
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PubMed id
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