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PDBsum entry 4omc
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Hydrolase/hydrolase inhibitor
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PDB id
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4omc
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References listed in PDB file
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Key reference
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Title
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X-Ray structures of human furin in complex with competitive inhibitors.
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Authors
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S.O.Dahms,
K.Hardes,
G.L.Becker,
T.Steinmetzer,
H.Brandstetter,
M.E.Than.
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Ref.
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Acs Chem Biol, 2014,
9,
1113-1118.
[DOI no: ]
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PubMed id
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Abstract
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Furin inhibitors are promising therapeutics for the treatment of cancer and
numerous infections caused by bacteria and viruses, including the highly lethal
Bacillus anthracis or the pandemic influenza virus. Development and improvement
of inhibitors for pharmacological use require a detailed knowledge of the
protease's substrate and inhibitor binding properties. Here we present a novel
preparation of human furin and the first crystal structures of this enzyme in
complex with noncovalent inhibitors. We show the inhibitor exchange by soaking,
allowing the investigation of additional inhibitors and substrate analogues.
Thus, our work provides a basis for the rational design of furin inhibitors.
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