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PDBsum entry 1qxk
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Contents |
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* Residue conservation analysis
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References listed in PDB file
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Key reference
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Title
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Identification of a monoacid-Based, Cell permeable, Selective inhibitor of protein tyrosine phosphatase 1b.
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Authors
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Z.Xin,
G.Liu,
C.Abad-Zapatero,
Z.Pei,
B.G.Szczepankiewicz,
X.Li,
T.Zhang,
C.W.Hutchins,
P.J.Hajduk,
S.J.Ballaron,
M.A.Stashko,
T.H.Lubben,
J.M.Trevillyan,
M.R.Jirousek.
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Ref.
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Bioorg Med Chem Lett, 2003,
13,
3947-3950.
[DOI no: ]
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PubMed id
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Abstract
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Monoacid-based PTP1B inhibitors with improved physiochemical properties have
been investigated. A (2-hydroxy-phenoxy) acetic acid-based phosphotyrosyl
mimetic has been linked with an optimized second arylphosphate binding site
ligand to produce compound 20 with low micromolar potency against PTP1B, good
selectivity over TCPTP (20-fold) and high cell permeability in the Caco-2 system.
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