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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.
|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.
Eelke van der Horst (project D1-105)
Drugs, Structures, Fragments
Marijn Sanders (project D1-105)
Design and application of structure-basedpharmacophores for class A GPCRs
Enade Perdana Istyastono (project D1-105)
Computational Studies of the Histamine H4 Receptor-Ligand Interactions
Anne Watts (project D1-105)
Dimeritization and signaling of the chemokine receptors CXCR3 and CCX-CKR
Danny Scholten (project D1-105)
Chemokine Receptors CXCR3 and CXCR7: Allosteric Ligand Binding, Biased Signaling, and Receptor Regulation