Dissertation
From every angle: novel insights into CC chemokine receptor 2 pharmacology
The CC chemokine receptor 2 (CCR2), a member of the G protein-coupled receptor (GPCR) superfamily, is widely involved in autoimmune and inflammatory diseases. However, no drugs for this receptor have made it to the pharmaceutical market yet.
- Author
- L.S. den Hollander
- Date
- 25 September 2024
- Links
- Thesis in Leiden Repository
In this thesis, the aim was to better understand CCR2 pharmacology to aid in drug discovery efforts. I discuss pharmacological characterization of the intracellular allosteric binding sites, as well as the sodium ion binding site of CCR2. In addition, the effect of cancer-associated mutations in CCR2 on receptor function and ligand effect, as well as the development of a novel affinity-based probe for the receptor are described. To obtain successful CCR2-targeting treatments, further attention should be paid to personalized medicine, exploitation of allosteric binding sites and novel methods to visualize CCR2. In this thesis, important steps have been taken to promote further CCR2-targeted drug development to cure a wide variety of CCR2-related diseases.