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Advancing therapeutics using antibody-induced dimerization of receptor tyrosine phosphatases

Michel L Tremblay1

  • 1Department of Biochemistry, Goodman Cancer Institute, Faculty of Medicine, McGill University, Montreal, Quebec H3A1A3, Canada michel.tremblay@mcgill.ca.

Genes & Development
|September 6, 2023
PubMed

Insights

Researchers developed a monoclonal antibody targeting PTPRD, inducing dimerization and inhibiting its activity. This antibody triggers PTPRD proteolysis, offering a new strategy for treating diseases linked to receptor protein tyrosine phosphatases (RPTPs).

Area of Science:

  • Molecular Biology
  • Cellular Biology
  • Immunology

Background:

  • Receptor protein tyrosine phosphatases (RPTPs) regulate crucial cellular processes.
  • Dysregulation of RPTPs is implicated in human diseases like cancer and neurological disorders.
  • Targeting RPTPs offers therapeutic potential for various pathologies.

Purpose of the Study:

  • To identify a novel therapeutic strategy for modulating PTPRD activity.
  • To investigate the effects of targeting the extracellular domain of PTPRD.
  • To explore the potential of antibody-mediated PTPRD inhibition.

Main Methods:

  • Development and application of a monoclonal antibody against PTPRD.
  • Analysis of antibody-induced PTPRD dimerization and phosphatase inhibition.
  • Investigation of PTPRD proteolysis via intracellular degradation pathways.

Main Results:

  • A monoclonal antibody successfully targeted the extracellular domain of PTPRD.
  • Antibody binding induced PTPRD dimerization and inhibited its phosphatase activity.
  • Dimeric PTPRD underwent proteolysis through intracellular degradation mechanisms.

Conclusions:

  • Modulating PTPRD via its extracellular domain is a viable therapeutic approach.
  • Antibody-mediated inhibition and subsequent degradation of PTPRD presents a new clinical strategy.
  • This study opens avenues for manipulating PTPRD and related phosphatases for disease treatment.
Keywords:
PTPRDSRCbivalent antibodydimerizationprotein tyrosine phosphorylationreceptor protein tyrosine phosphatase

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