Challenges in the development of heteromer-GPCR-based drugs

Prog Mol Biol Transl Sci. 2013:117:143-62. doi: 10.1016/B978-0-12-386931-9.00006-4.

Abstract

G-protein-coupled receptors are targets of a variety of diseases. Drug screening has been classically performed assuming the occurrence of monomeric receptors. As more and more receptor heteromers are identified, the challenge is now to develop screening assays to select heteromer-specific drugs. These drugs may, for instance, be able to interact preferentially with prerather than with postsynaptic receptors. Heteromer-based drug discovery opens new perspectives in both Academic pursuits and for the Pharmaceutical industry.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Allosteric Regulation
  • Animals
  • Drug Discovery*
  • Humans
  • Molecular Targeted Therapy
  • Pharmaceutical Preparations / metabolism*
  • Protein Multimerization*
  • Receptors, G-Protein-Coupled / metabolism*

Substances

  • Pharmaceutical Preparations
  • Receptors, G-Protein-Coupled