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Structure‐Based Optimization of Benzoic Acids as Inhibitors of Protein Tyrosine Phosphatase 1B and Low Molecular Weight Protein Tyrosine Phosphatase
Author(s) -
Maccari Rosanna,
Ottanà Rosaria,
Ciurleo Rosella,
Paoli Paolo,
Manao Giampaolo,
Camici Guido,
Laggner Christian,
Langer Thierry
Publication year - 2009
Publication title -
chemmedchem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.200800427
Subject(s) - protein tyrosine phosphatase , biochemistry , phosphatase , tyrosine , gene isoform , chemistry , enzyme , benzoic acid , gene
We have optimized previously discovered benzoic acids 1 , which are active as inhibitors of PTP1B and LMW‐PTP, two protein tyrosine phosphatases that have emerged as attractive targets for the development of novel therapeutic agents for the treatment of diabetes, obesity, and cancer. Our efforts led to the identification of new and more potent analogues with appreciable selectivity toward human PTP1B and the IF1 isoform of human LMW‐PTP.