Insights into Receptor Function and New Drug Development Targets

  • Conn Michael 
  • Kordon Claude 
  • Christen Yves 
Conference proceedings

Table of contents

  1. Front Matter
    Pages I-XV
  2. Shaun P. Brothers, P. Michael Conn
    Pages 23-33
  3. Cécile Lubrano, Béatrice Dubern, Karine Clément
    Pages 35-51
  4. Max Lafontan, Michel Berlan, Coralie Sengenes, Cédric Moro, François Crampes, Jean Galitzky
    Pages 53-77
  5. X. Iturrioz, A. Reaux-Le Goazigo, A. Hus-Citharel, N. De Mota, L. Bodineau, A. Frugière et al.
    Pages 79-92
  6. J. P. Pin, C. Goudet, J. Kniazeff, V. Hlavackova, C. Brock, V. Binet et al.
    Pages 105-115
  7. J. Rivier, J. Gulyas, J. Erchegyi, S. C. Koerber, C. R. R. Grace, R. Riek et al.
    Pages 117-138
  8. Gilbert Vassart, Leonardo Pardo, Sabine Costagliola
    Pages 151-166
  9. Andreas Gschwind, Oliver M. Fischer, Axel Ullrich
    Pages 167-178
  10. Shlomo Melmed
    Pages 179-187
  11. Back Matter
    Pages 201-202

About these proceedings


G-Protein Coupled receptors (GPCRs) and other receptors are significant targets for drug discovery, due to their roles in fundamental physiological processes. Among these roles are: regulation of growth, food intake, reproduction, water balance, sensory perception, blood pressure and heart rate. GPCR-directed drugs account for approximately $40 billion in sales and, of drugs at market, approximately 70% target GPCR function.

The availability of combinatorial chemistry coupled with high throughput screening techniques have facilitated discovery of peptidic and non-peptidic ligands of membrane receptors. Mutant receptor models have revealed their role in health and disease and provided insight to new therapeutic approaches, based on control of protein trafficking. Understanding receptor-receptor interactions has provided one mechanism for receptor cross-talk and revealed unexpected interactions.

The completion of the human genome has identified a new source of therapeutic targets: "orphan receptors" with unknown functions and yet-to-be discovered ligands. Some orphans have now been identified as ghrelin, nociceptin, apelin, and urocortin. This finding, along with important technologies to develop ligands with desirable characteristics, including peptidomimetics is likely to further accelerate interest in this area.


Cannabinoid G protein-coupled receptors G proteins RGS proteins TRPC channels endogenous cannabinoid system glycoprotein hormone receptors hormone receptors ion channels lipolysis melanocortin receptors metabotropic glutamate receptors receptor tyrosine kinases

Editors and affiliations

  • Conn Michael 
    • 1
  • Kordon Claude 
    • 2
  • Christen Yves 
    • 3
  1. 1.Divisions of Neuroscience and Reproductive Biology, Departments of Physiology and Pharmacology and Cell and Developmental BiologyOregon National Primate Research Center, Oregon Health and Science UniversityBeavertonUSA
  2. 2.Institut NeckerParisFrance
  3. 3.Pour la Recherche ThérapeutiqueFondation IPSENParis Cedex 16France

Bibliographic information