One of the most commonly used and successful targets for drugs is a specific protein group in human cells called G protein-coupled receptors (GPCRs). In fact approximately forty to fifty percent of all modern medicines interact with this protein group. Due to their physiological and pathophysiological relevance, these GPCRs are prime targets of interest for both academia and the pharmaceutical industry.

This project brings together researchers from a wide variety of disciplines, from physics to informatics, to develop new concepts for the measurement and modulation of GPCR activity. So far new methods have been developed that make a more specific approach to GPCRs possible, thus decreasing possible side effects of identified ligands.

Fast facts 

Full project title:The GPCR Forum: novel concepts and tools for established targets
Start date: August 2007
End date: August 2011
Goal: Develop new strategies to measure and specify the activity of ligands interacting with GPCRs
Principal investigator: Ad IJzerman, Leiden University
Project size: 27 FTE's
Partners: Leiden University, MSD, Abbott, University Medical Center Groningen, University Medical Center Utrecht, University Medical Center Nijmegen, VU University Amsterdam


G protein-coupled receptors are a large family of membrane proteins and are an important class of receptors. There are more than 5000 variants of this receptor, active in practically all organs. Despite this variety they function according to the same principles. The receptors can ‘feel’ molecules outside of the cell and activate signal-transduction mechanisms inside the cell therewith activating a cellular response. For example, the GPCR in the eye can detect that light enters the eye, gives a signal through the cell membrane which consequently leads to a nerve signal to the brain.

GPCR’s role as contributor to the information flow into cells also makes that they are associated with a multitude of diseases. To date they are therefore the most important group of target molecules for the pharmaceutical industry; more than 40% of all drugs have a GPCR as target. This prominent role of GPCR in drug development will, most likely, not diminish in the near future but rather increase.

PhD theses from this project

Eelke van der Horst (project D1-105)
Drugs, Structures, Fragments

Miriam Peeters (project D1-105)
Activation of G-protein-coupled Receptors

Clara Blad (project D1-105)
A quest for connections

“One of TI Pharma's big strengths is that it knows how to manage money. That's a skill that should be more widespread.”

Tim Wells
Chief Scientific Officer
Medicines for Malaria Venture

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