Communication

Structure-Based Optimization of Benzoic Acids as Inhibitors of Protein Tyrosine Phosphatase 1B and Low Molecular Weight Protein Tyrosine Phosphatase

  1. Rosanna Maccari Dr.1,
  2. Rosaria Ottanà Prof.1,
  3. Rosella Ciurleo Dr.1,
  4. Paolo Paoli Dr.2,
  5. Giampaolo Manao Prof.2,
  6. Guido Camici Prof.2,5,
  7. Christian Laggner Dr.3,
  8. Thierry Langer Prof.4

Article first published online: 13 MAR 2009

DOI: 10.1002/cmdc.200800427

Issue

ChemMedChem

ChemMedChem

Special Issue: XIX NMMC Verona 2008

Volume 4, Issue 6, pages 957–962, June 8, 2009

Additional Information

How to Cite

Maccari, R., Ottanà, R., Ciurleo, R., Paoli, P., Manao, G., Camici, G., Laggner, C. and Langer, T. (2009), Structure-Based Optimization of Benzoic Acids as Inhibitors of Protein Tyrosine Phosphatase 1B and Low Molecular Weight Protein Tyrosine Phosphatase. ChemMedChem, 4: 957–962. doi: 10.1002/cmdc.200800427

Author Information

  1. 1

    Dipartimento Farmaco-chimico, Università di Messina, Polo Universitario Annunziata, 98168 Messina (Italy), Fax: (+39) 90-676-6402

  2. 2

    Dipartimento di Scienze Biochimiche, Università di Firenze, Viale Morgagni 50, 50134 Firenze (Italy)

  3. 3

    Department of Pharmaceutical Chemistry, Institute of Pharmacy and Center for Molecular Biosciences (CMBI), University of Innsbruck, Innrain 52c, 6020 Innsbruck (Austria)

  4. 4

    Prestwick Chemical Inc. Bld. Gonthier d'Andernach, 67400 Strasbourg–Illkirch (France)

  5. 5

    Center of Excellence for Scientific Research DENOTHE, Viale Morgagni 44, 50134 Firenze (Italy)

Publication History

  1. Issue published online: 28 MAY 2009
  2. Article first published online: 13 MAR 2009
  3. Manuscript Revised: 17 JAN 2009
  4. Manuscript Received: 12 DEC 2008

Funded by

  • FIRB 2003-project. Grant Number: RBNE03FMCJ_007
  • University of Messina. Grant Number: PRA 2005

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Keywords:

  • benzoic acids;
  • drug design;
  • enzymes;
  • inhibitors;
  • protein tyrosine phosphatases

Abstract

Thumbnail image of graphical abstract

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.

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