Cannabinoid receptor 2 as a ‘drugable’ target: kinetic profile of novel receptor ligands
Supervisor: Andrea Martella
- Laura Heitman
The discovery of Δ 9-THC, the main psychoactive molecule in cannabis plants, and the following characterization of cannabinoid receptors in several parts of the human body, set the basis for a whole new research field. Cannabinoid receptors 1 and 2, and their endogenous ligands (i.e. endocannabinoids), are present in almost all the animal species and are involved in a wide range of diseases. These two receptors are part of the rhodopsin-like G protein-coupled receptor family. Cannabinoid receptor 2 (CB2R) is mainly expressed in immune tissues with almost no expression in the central nervous system. These features make the CB2R a potential drug target for a wide variety of human diseases ranging from heart and kidney disorders to osteoporosis and neuropathic pain.
In order to characterize and select novel CB2R ligands, affinity and kinetic studies will be performed during our compound selection process. The binding kinetic profile of a certain drug provides important information about how long a ligand stays on the target receptor, and generally this feature is linked to its in vivo potency. The possibility to describe the behavior of a drug in an in vivo scenario increase the chances to develop a compound that will succeed during the later stages of the research and development (R&D) process.
Therefore, the aim of this project is to study with in vitro techniques the ligand binding behavior on CB2R, with the prospect to better evaluate the in vivo efficacy of a certain drug. To accomplish this objective we need motivated bachelor and master students that are willing to be involved in a challenging and multi-disciplinary project.
- Cell culture
- Radioligand binding assays
- Functional assays