• Corpus ID: 82681533

Regulation and Pharmacological Manipulation of the Type 5 Metabotropic Glutamate (mGlu5) Receptor

  title={Regulation and Pharmacological Manipulation of the Type 5 Metabotropic Glutamate (mGlu5) Receptor},
  author={Sophie J. Bradley},
Coopman, K., Bradley, S.J., Wilkinson, G.F. and Willars, G.B. G-protein coupling and glucagonlike peptide-1 signalling in recombinant cell-lines. 2 Focused Meeting Cell Signalling 16-17 April 2007. Poster Presentation. Bradley, S.J., Howes, C.M., Wood, M.D. and Challiss, R.A.J. Effects of Positive Allosteric Modulators of the mGlu5 Receptor on Oscillatory Patterns of Ca 2+ Signalling. Metabotropic glutamate receptor conference Sicily 14-19 September 2008. Poster Presentation. Bradley, S.J… 



Structural, signalling and regulatory properties of the group I metabotropic glutamate receptors: prototypic family C G-protein-coupled receptors.

This review will focus on the group I mGlu receptors, a subgroup of receptors that is widely and differentially expressed in neuronal and glial cells within the brain, and receptor activation has been implicated in the control of an array of key signalling events.

Control of calcium oscillations by phosphorylation of metabotropic glutamate receptors

It is reported that glutamate induces single-peaked intracellular Ca2+ mobilization in mGluR1α-transfected cells but elicits Ca2- oscillations in m gluR5a-expressing cells, the first evidence that PKC phosphorylation of G-protein-coupled receptors is important in producing oscillations of Ca2 + signalling.

Regulation of metabotropic glutamate receptor signaling, desensitization and endocytosis.

Norbin Is an Endogenous Regulator of Metabotropic Glutamate Receptor 5 Signaling

It is reported that Norbin, a neuron-specific protein, physically interacts with mGluR5 in vivo, increases the cell surface localization of the receptor, and positively regulates mGLUR5 signaling.

Effects of Positive Allosteric Modulators on Single-Cell Oscillatory Ca2+ Signaling Initiated by the Type 5 Metabotropic Glutamate Receptor

It is demonstrated that allosteric modulators can “tune” the Ca2+ oscillation frequency initiated by mGlu5 receptor activation, and this might allow pharmacological modification of the downstream processes (e.g., transcriptional regulation) that is unachievable through orthosteric ligand interactions.

The Metabotropic Glutamate Receptor mGluR5 Induces Calcium Oscillations in Cultured Astrocytes via Protein Kinase C Phosphorylation

It is demonstrated that mGluR5 is capable of inducing [Ca2+]i oscillations in cultured astrocytes and that phosphorylation/dephosphorylation of mGlamorganic glutamate receptor is critical in [Ca1+] i oscillations, analogous to the cloned mGLUR5 expressed in heterologous cell lines.