Engineering Diptheria Toxin Towards the Development of Therapeutics against Breast Cancer

Abstract

The goal of this project is to design a cytotoxic protein using diphtheria toxin as a template that will recognize and bind to a cell that overproduces heregulin (HRG) precursor on the cell surface. HRG is an activating growth factor ligand for HER-4, whose overexpression is correlated with breast cancer cells. Given the recent success with the humanized monoclonal antibody (herceptin) against erb-B receptors as therapeutics against breast cancer, we hypothesize that the downregulation of the production of this ligand will lead to the inhibition of the growth of breast cancer cells. In 1997, we have completed the crystal structure of diphtheria toxin (DT) complexed with an extracellular fragment of its receptor protein, a membrane- bound precursor of human heparin-binding EGF (HBEGF). HBEGF is structurally homologous to HRG, thus providing a point of departure for molecular design of diphtheria toxin in order to divert to a new target receptor, HRG. The engineered toxin will be tested in vivo for its efficiency in targeted delivery of cytotoxicity.

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Document Details

Document Type
Technical Report
Publication Date
Sep 01, 1998
Accession Number
ADA377811

Entities

People

  • Senyon Choe

Organizations

  • Salk Institute for Biological Studies

Tags

DTIC Thesaurus Topics

  • Amino Acids
  • Biological Factors
  • Blood Coagulation Factors
  • Breast Cancer
  • Cell Physiological Processes
  • Cells
  • Chemistry
  • Crystal Structure
  • Crystals
  • Growth Factors
  • Lymphocytes
  • Molecules
  • Neoplasms
  • Peptide Growth Factors
  • Peptides
  • Proteins
  • Therapy

Fields of Study

  • Biology

Readers

  • Breast cancer cell signaling and growth regulation.
  • Molecular and Cellular Biochemistry