Structure-based optimization of benzoic acids as inhibitors of protein tyrosine phosphatase 1B and low molecular weight protein tyrosine phosphatase

Rosanna Maccari, Rosaria Ottanà, Rosella Ciurleo, Paolo Paoli, Giampaolo Manao, Guido Camici, Christian Laggner, Thierry Langer

Research output: Contribution to journalArticle

Abstract

(Chemical Equation Presented) 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.

Original languageEnglish
Pages (from-to)957-962
Number of pages6
JournalChemMedChem
Volume4
Issue number6
DOIs
Publication statusPublished - Jun 8 2009

Keywords

  • Benzoic acids
  • Drug design
  • Enzymes
  • Inhibitors
  • Protein tyrosine phosphatases

ASJC Scopus subject areas

  • Molecular Medicine
  • Organic Chemistry
  • Pharmacology, Toxicology and Pharmaceutics(all)

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