The 5-HT6 receptor interactome: new insight in receptor signaling and its impact on brain physiology and pathologies.

The 5-HT6 receptor interactome: new insight in receptor signaling and its impact on brain physiology and pathologies. Neuropharmacology. 2019 Nov 01;:107839 Authors: Chaumont-Dubel S, Dupuy V, Bockaert J, Bécamel C, Marin P Abstract The serotonin (5-HT)6 receptor is a Gs-coupled receptor exclusively expressed in the central nervous system. Highest receptor densities are found in brain regions implicated in mnemonic functions where the receptor is primarily but not exclusively located in the primary cilium of neurons. The 5-HT6 receptor continues to raise particular interest for neuropharmacologists, given the pro-cognitive effects of antagonists in a wide range of cognitive impairment paradigms in rodents and human. The 5-HT6 receptor also finely controls key neuro-developmental processes including neuron migration and differentiation. However, its influence upon neurodevelopment and cognition is not solely mediated by its coupling to the Gs-adenylyl cyclase pathway, suggesting alternative signal transduction mechanisms. This prompted studies aimed at characterizing the receptor interactome that identified 125 candidate receptor partners, making the 5-HT6 receptor one of the G protein-coupled receptors with the most extensively characterized interactome. These studies showed that the receptor localization at the plasma membrane and, consequently, its signal transduction, are finely modulated by several receptor partners. They demons...
Source: Neuropharmacology - Category: Drugs & Pharmacology Authors: Tags: Neuropharmacology Source Type: research