It's about time: novel drug discovery concepts for the molecular pharmacological characterization fo the cannabinoid CB2 receptor

Abstract

This thesis explored the molecular pharmacological mechanisms of targeting CB2R via investigation of novel drug discovery concepts such as target binding kinetics, allosteric modulation and biased signaling. Central to the investigation of CB2R pharmacology was developing new assays and providing an overall kinetic view, aimed at bringing fresh insights that could be further integrated into the field of GPCR research. To this end, the development and application of state-of-the-art and novel cellular and biochemical assays contributed to a better understanding of agonist-mediated CB2R activation and signaling, which can advance drug discovery efforts for treatments of diseases that involve CB2R.

It’s about time that novel concepts for GPCRs are incorporated into early drug discovery programs, where a kinetic view is applied to provide a better translational perspective.