G protein-coupled receptors: from structures to funtionally validated targets (GPCRs)

  • Steyaert, Jan (Administrative Promotor)
  • Proost, Paul (Co-Promotor)
  • Thevelein, Johan (Co-Promotor)
  • Van Damme, J. (Co-Promotor)
  • Vanden Broeck, Jozef (Co-Promotor)
  • Parmentier, Marc (Co-Promotor)
  • Desmecht, Daniel (Co-Promotor)

Project Details


G protein-coupled receptors (GPCR) represent the largest family among membrane receptors. These receptors and their structurally diverse ligands play a major role in all aspects of physiology and pathophysiology, and constitute the targets for about half the active compounds presently used as therapeutic agents. While GPCRs were long thought to function as monomers, it is currently accepted that GPCRs form homo- and/or hetero-complexes and are anchored in membrane regions with specific lipid/(glyco)protein components. These contextual factors modulate signalling and can cause disease-specific receptor dysregulations. Partners of the present programme have played a major role in the characterization of many G protein-coupled receptors and their ligands in different species. The GPCR field is now at an exciting phase of its evolution. Indeed, structural data become available at a rapidly increasing pace, and this will affect deeply all other aspects of the field. Based on the network's previous experience, and thanks to new partners and external collaborations worldwide, we intend to remain at the forefront of GPCR research by performing world class investigations into novel directions taken by the field. With a new focus onto structural aspects, we will study further both general and specific aspects of GPCRs, with the ultimate goal of improving human health and quality of life.
Effective start/end date1/04/1230/09/17


  • Applied Biology

Flemish discipline codes

  • Systems biology
  • Allosteric coupling from G protein to the agonist-binding pocket in GPCRs

    DeVree, B. T., Mahoney, J. P., Vélez-Ruiz, G. A., Rasmussen, S. G. F., Kuszak, A. J., Edwald, E., Fung, J-J., Manglik, A., Masureel, M., Du, Y., Matt, R. A., Pardon, E., Steyaert, J., Kobilka, B. K. & Sunahara, R. K., 7 Jul 2016, In : Nature. 535, 7610, p. 182-186 5 p.

    Research output: Contribution to journalArticle

    Open Access
    150 Citations (Scopus)
    285 Downloads (Pure)