Expression-driven reverse engineering of targeted imaging and therapeutic agents

Expert Opin Ther Targets. 2003 Apr;7(2):137-9. doi: 10.1517/14728222.7.2.137.


Cancer is a particularly daunting disease to treat because, in its most insidious forms, cells are disseminated throughout the body, rendering surgery and local therapies ineffective. Hence, systemic disease must be targeted by its metabolic, physiological or molecular phenotype rather than by its location. Both tumour metabolism and physiology have been exploited to target therapies with some success. There is every reason to expect that these approaches will continue to advance therapies that discriminate tumour metabolism from that of normal tissues. As an alternative, molecular phenotyping (pharmacogenomics) is a relatively new science, and holds great promise for development of novel therapies and approaches. The discipline of pharmacogenomics has, to date, involved segmentation of patients according to their protein expression patterns in order to direct existing therapies to those populations who stand to benefit the most. In this communication, the authors propose a further application of this technology to develop agents that are reverse-engineered to explicitly target a patient's expressed protein patterns.

Publication types

  • Editorial
  • Research Support, N.I.H., Extramural
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Antigen-Antibody Reactions
  • Antineoplastic Agents
  • Biopolymers
  • Chemical Phenomena
  • Chemistry, Physical
  • Drug Delivery Systems / methods*
  • Drug Design*
  • Epitopes / chemistry
  • Gene Expression Profiling
  • Gene Expression*
  • Genetic Engineering / methods*
  • Humans
  • Individuality
  • Ligands
  • Molecular Structure
  • Pharmacogenetics / methods*
  • Phenotype
  • Protein Binding
  • Receptors, Cell Surface / drug effects
  • Receptors, Cell Surface / metabolism
  • Structure-Activity Relationship


  • Antineoplastic Agents
  • Biopolymers
  • Epitopes
  • Ligands
  • Receptors, Cell Surface