GRM1 Membrane Protein Introduction

Introduction of GRM1

The metabotropic glutamate receptor 1 (also known as mGluR1, GRM1) is a member of the group I metabotropic glutamate receptors (mGluRs), which are family C G-protein coupled receptors that participate in the modulation of synaptic transmission and neuronal excitability throughout the central nervous system. Like other mGluRs, this receptor has a large extracellular domain, which binds to the glutamate and mediates cell signal transduction. GRM1 is widely expressed in the neurons and taste buds. The activation of GRM1 can result in phospholipase C stimulation, adenylyl cyclase stimulation, and adenosine monophosphate (MAP) kinase phosphorylation.

Functions of GRM1 Membrane Protein

GRM1 has been genetically deleted in mice to study the potential roles in cell function and in various disease states. These animals show normal gross brain morphology, but they exhibit abnormal induction of long-term potentiation (LTP) and they are unable to learn the associative task. Moreover, they showed significant impairments in the ability to induce LTP and cerebellar gait problems. As a result, it is a crucial pharmacological target for several central nervous system disorders. Moreover, GRM1 activation at the onset of reperfusion induces cardioprotection and might represent a putative strategy to prevent ischemia-reperfusion injury. Mutations in the GRM1 gene may contribute to melanoma susceptibility. A number of potent and specific allosteric ligands have been developed for various studies.

Applications of GRM1 Membrane Protein in Literature

1. Jiang L., et al. Virtual screening and molecular dynamics study of potential negative allosteric modulators of mGluR1 from Chinese herbs. Molecules. 2015, 20(7): 12769-12786. PubMed ID: 26184151
   
   

   In this article, a series of computer-aided drug design methods were utilized to discover potential mGluR1 negative allosteric modulators from Chinese herbs.

2. Bakshi K., et al. Prenatal cocaine exposure uncouples mGluR1 from Homer1 and Gq Proteins. Plos One. 2014, 9(3): e91671. PubMed ID: 24626340
   
   

   Since mGluR1 was a pivotal regulator of the glutamatergic neurotransmission and cognitive processes, this article investigated the effect of prenatal cocaine exposure on signaling dysfunction in the mGluR1 system and the underlying mechanisms.

3. Yamasaki T., et al. In vivo monitoring for regional changes of metabotropic glutamate receptor subtype 1 (mGluR1) in pilocarpine-induced epileptic rat brain by small-animal PET. Scientific Reports. 2017, 7(1): 14945. PubMed ID: 29097780
   
   

   This article investigated the functions of mGluR1 in neuroexcitotoxicity. The investigators monitored in vivo regional changes of mGluR1 related to neuroinflammation in the brains of rats after pilocarpine-induced status epilepticus using longitudinal positron emission tomography.

4. Zhou C. H., et al. SIRT1 attenuates neuropathic pain by epigenetic regulation of mGluR1/5 expressions in type 2 diabetic rats. Pain. 2017, 158(1): 130. PubMed ID: 27749604
   
   

   The investigators examined the role of spinal SIRT1 in T2DM-induced neuropathic pain and explored its underlying mechanism. Results showed that the activation of SIRT1 with SIRT1 agonist can functionally reverse pain behavior and epigenetically downregulate the expressions of mGluR1/5.

5. Zhao Y., et al. Involvement of mGluR I in EphB/ephrinB reverse signaling activation induced retinal ganglion cell apoptosis in a rat chronic hypertension model. Brain Research. 2018, 1683. PubMed ID: 29366625
   
   

   This article investigated the mechanisms underlying EphB/ephrinB reverse signaling activation induced RGC apoptosis in a rat chronic ocular hypertension (COH) model. Results showed that mGluR1 may be one of the key targets when EphB/ephrinB reverse signaling was activated, and over-activation of mGluR1 may contribute to RGC apoptosis in COH retina.

GRM1 Preparation Options

The study of membrane proteins is challenging due to the difficulties to extract them from their natural environment and subsequently maintain them in stable, water-soluble form. With a particular focus on this field, Creative Biolabs has developed a powerful Magic™ Membrane Protein Production Platform to prepare membrane proteins in different functional formats. We have rich experience in preparing various classes of membrane proteins, including GPCRs, ion channels, transporters, etc. In response to our clients’ diverse uses and applications of the target membrane protein, we offer multiple reconstitution systems to meet every specific research requirement. Aided by our versatile Magic™ anti-membrane protein antibody discovery platform, we also provide customized anti-GRM1 antibody development services.

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