Structural Basis of Metabotropic Glutamate Receptor 5 (mGlu5) Allosteric Modulation

The metabotropic glutamate receptor subtype 5 (mGlu5) is a transmembrane spanning class C G protein coupled receptor (GPCR). Understanding differential effects of allosteric modulators on stabilising distinct receptor conformations both in human and non-human species with physiologically related signalling endpoints linked to therapeutic efficacy and avoid on-target adverse effects. The obvious and immense potential of modulators of glutamatergic neurotransmission in a wide range of CNS disorders attract pharmacologists to design small molecules not only as prospective therapies, but also pharmacological tools for improve understanding of the structural basis of allosteric modulation observed in mGlu5 dimers.