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PDBsum entry 1xbo
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References listed in PDB file
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Key reference
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Title
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Isoxazole carboxylic acids as protein tyrosine phosphatase 1b (ptp1b) inhibitors.
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Authors
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H.Zhao,
G.Liu,
Z.Xin,
M.D.Serby,
Z.Pei,
B.G.Szczepankiewicz,
P.J.Hajduk,
C.Abad-Zapatero,
C.W.Hutchins,
T.H.Lubben,
S.J.Ballaron,
D.L.Haasch,
W.Kaszubska,
C.M.Rondinone,
J.M.Trevillyan,
M.R.Jirousek.
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Ref.
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Bioorg Med Chem Lett, 2004,
14,
5543-5546.
[DOI no: ]
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PubMed id
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Abstract
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Guided by X-ray crystallography, we have extended the structure-activity
relationship (SAR) study on an isoxazole carboxylic acid-based PTP1B inhibitor
(1) and more potent and equally selective (>20-fold selectivity over the
highly homologous T-cell PTPase, TCPTP) PTP1B inhibitors were identified.
Inhibitor 7 demonstrated good cellular activity against PTP1B in COS 7 cells.
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