Delineating the stepwise millisecond allosteric activation mechanism of the class C GPCR dimer mGlu5

M Li, X Lan, X Shi, C Zhu, X Lu, J Pu, S Lu… - Nature …, 2024 - nature.com
Two-thirds of signaling hormones and one-third of approved drugs exert their effects by
binding and modulating the G protein-coupled receptors (GPCRs) activation. While the …

Pharmacology, Signaling and Therapeutic Potential of Metabotropic Glutamate Receptor 5 Negative Allosteric Modulators

JA Kos, M Langiu, SD Hellyer… - ACS Pharmacology & …, 2024 - ACS Publications
Metabotropic glutamate receptors are a family of eight class CG protein-coupled receptors
regulating higher order brain functions including cognition and motion. Metabotropic …

Pharmacological characterisation of allosteric modulators at human mGlu5

M Razzak, K Tran, R McCague, K Sengmany, J Kos… - bioRxiv, 2024 - biorxiv.org
The metabotropic glutamate receptor 5 (mGlu5) is a Class CG protein-coupled receptor,
ubiquitously expressed throughout the CNS. With major roles in cognition, learning and …