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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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References listed in PDB file
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Key reference
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Title
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Acetylenic tace inhibitors. Part 3: thiomorpholine sulfonamide hydroxamates.
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Authors
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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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Ref.
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Bioorg Med Chem Lett, 2006,
16,
1605-1609.
[DOI no: ]
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PubMed id
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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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