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PDBsum entry 2a95
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Membrane protein
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PDB id
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2a95
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DOI no:
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Bioorg Med Chem Lett
16:1605-1609
(2006)
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PubMed id:
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Acetylenic TACE inhibitors. Part 3: Thiomorpholine sulfonamide hydroxamates.
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J.I.Levin,
J.M.Chen,
L.M.Laakso,
M.Du,
J.Schmid,
W.Xu,
T.Cummons,
J.Xu,
G.Jin,
D.Barone,
J.S.Skotnicki.
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ABSTRACT
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A series of thiomorpholine sulfonamide hydroxamate TACE inhibitors, all bearing
propargylic ether P1' groups, was explored. In particular, compound 5h has
excellent in vitro potency against isolated TACE enzyme and in cells, oral
activity in a model of TNF-alpha production and a collagen-induced arthritis
model, was selected as a clinical candidate for the treatment of RA.
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Literature references that cite this PDB file's key reference
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PubMed id
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Reference
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M.S.Bahia,
and
O.Silakari
(2010).
Tumor necrosis factor alpha converting enzyme: an encouraging target for various inflammatory disorders.
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Chem Biol Drug Des,
75,
415-443.
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The most recent references are shown first.
Citation data come partly from CiteXplore and partly
from an automated harvesting procedure. Note that this is likely to be
only a partial list as not all journals are covered by
either method. However, we are continually building up the citation data
so more and more references will be included with time.
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');
}
}
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