Structure-Based Discovery of Negative Allosteric Modulators of the Metabotropic Glutamate Receptor 5.

ABSTRACT: Recently determined structures of class C G protein-coupled receptors (GPCRs) revealed the location of allosteric binding sites and opened new opportunities for the discovery of novel modulators. In this work, molecular docking screens for allosteric modulators targeting the metabotropic glutamate receptor 5 (mGlu₅) were performed. The mGlu₅ receptor is activated by the main excitatory neurotransmitter of the nervous central system, L-glutamate, and mGlu₅ receptor activity can be allosterically modulated by negative or positive allosteric modulators. The mGlu₅ receptor is a promising target for the treatment of psychiatric and neurodegenerative diseases, and several allosteric modulators of this GPCR have been evaluated in clinical trials. Chemic

SUBMITTER: Kampen S 

PROVIDER: S-EPMC9594040 | biostudies-literature | 2022 Oct

REPOSITORIES: biostudies-literature