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Article

Probe dependence and biased potentiation of metabotropic glutamate receptor 5 is mediated by differential ligand interactions in the common allosteric binding site.

Biochemical pharmacology - 1 Jul 2020

Hellyer Shane D, Sengmany Kathy, Keller Andrew N, Christopoulos Arthur, Leach Katie, Gregory Karen J

Abstract excerpt

The metabotropic glutamate receptor 5 (mGlu5) is a promising therapeutic target for multiple CNS disorders. Recent mGlu5 drug discovery has focused on targeting binding sites within the mGlu5 7-transmembrane domain (7TM) that are topographically distinct from that of the endogenous ligand. mGlu5 primarily couples to Gq/11 proteins leading to mobilization of intracellular Ca2+ (iCa2+), but also activates iCa2+...

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PMID: 32389635
DOI: 10.1016/j.bcp.2020.114013

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