About this Research Topic
G-protein coupled receptors (GPCRs) represent the largest class of both human membrane proteins play critical roles in regulating brain function. GPCRs represent the most important targets in modern pharmacology because of the different functions they mediate, especially within brain and peripheral nervous system, and also because of their functional and stereochemical properties. However, ligands that selectively activate a single receptor subtype exist for only a small fraction of GPCRs and it has been difficult to develop highly selective ligands for most GPCR subtypes.
The objective of this Hot Topic is to bring together relevant international researchers from the GPCR field to preset up-to-date contributions on anatomical, biochemical, neuropharmacological, translational data addressing the actions of different GPCRs in the brain in the context of obesity, depression and epilepsy and other disorders of the CNS.
GPCR researchers with a range of expertise are welcome to submit their contributions. We particularly welcome submission on GPCR binding, protein activation, effector bias, receptors heterodimerization, positive (PAM) and negative (NAM) allosteric modulators, polypharmacology and others.
These are exciting times for GPCR researchers with the new discoveries that may provide several mechanistic advantages including the ability to distinguish between closely related receptor subtypes. Collectively, the new tools have the promise to provide unprecedented insights into the biology and circuitry underlying numerous CNS diseases. These discoveries will inform drug discovery efforts on how to optimally steer receptor signaling in a given patient population to provide maximal efficacy with minimal side-effects and provide exciting opportunities for the treatment of CNS orders.
Keywords: G-protein coupled receptors, PAM, PAN, Heterodimer, Polypharmacology, Clinical pharmacology, Neuroscience, Neurology
Important Note: All contributions to this Research Topic must be within the scope of the section and journal to which they are submitted, as defined in their mission statements. Frontiers reserves the right to guide an out-of-scope manuscript to a more suitable section or journal at any stage of peer review.