Allosteric molecular switches in metabotropic glutamate receptors

Zoltán Orgován, György G Ferenczy, György M Keseru
ChemMedChem 2020 July 19
Metabotropic glutamate receptors (mGlu) are class C G protein-coupled receptors and contain eight subtypes that are omnipresently expressed in the central nervous system. mGlus have relevance in several psychiatric and neurological disorders, therefore mGlus raised considerable interest as drug targets. Drug discovery programs mainly aimed to develop allosteric modulators targeting different mGlus that offer advantages over orthosteric ligands owing to their increased potential to achieve subtype selectivity that prompted discovery programs with a large number of allosteric mGlu ligands reported. However, the optimization of allosteric ligands into drug candidates proved to be challenging owing to induced fit effects, flat or steep structure activity relationship and unexpected changes in their functional activity. The latters are identified as allosteric molecular switches in glutamate receptor family and are reviewed here.

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