CHRM2 Membrane Protein Introduction

Introduction of CHRM2

CHRM2, encoded by CHRM2 gene, is a member of G protein-coupled receptors family which has seven distinctive transmembrane domains. It is one of the five subtypes of muscarinic receptors (CHRM1-5), selectively expressed in various human tissues, including heart, gallbladder, and 3 other tissues. Research have found that muscarinic receptors are the potential therapeutic targets for a variety of pathological conditions, especially in neurodegenerative disorders.

Function of CHRM2 Membrane Protein

CHRM2 can bind acetylcholine thereby regulating various cellular responses, including the decrease of cAMP, phosphoinositide degeneration as well as potassium channels mediation. Moreover, it plays a critical role in a great number of important central and peripheral physiological and pathophysiological processes. It has been shown that CHRM2 is involved in the mediation of bradycardia and a decrease in cardiac contractility. Besides, CHRM2 plays a key role in facilitating cognitive processes. The deficiency of CHRM2 in mice may present deficits in behavioral flexibility, working memory, and hippocampal plasticity. And multiple SNPs across CHRM2 are associated with adult performance IQ. In addition, the discoveries show that CHRM2 is associated with the progression of multiple diseases, such as Alzheimer disease, familial dilated cardiomyopathy, early adolescents’ depression, and asthma. These also suggest that CHRM2 can be considered as a potential therapeutic target for many diseases treatment.

Fig.1 The structure of CHRM2.

Application of CHRM2 Membrane Protein in Literature

1. Liu Y L., et al. Feishu acupuncture inhibits acetylcholine synthesis and restores muscarinic acetylcholine receptor M2 expression in the lung when treating allergic asthma. Inflammation. 2018, 41(3): 741-750. PubMed ID: 29520557
   
   

   The research confirms that Feishu acupuncture can relieve allergic asthma. The mechanisms may be involved in the suppression of the Ach signal both from its synthesis and during its release.

2. Solismaa A., et al. Genetic polymorphisms associated with constipation and anticholinergic symptoms in patients receiving clozapine. J Clin Psychopharmacol. 2018, 38(3): 193-199. PubMed ID: 29620694
   
   

   The study reveals that a genetic-risk score (GRS) of 9 SNPs in CHRM2, CHRM3, HTR3C, HTR7, ABCB1, OPRM1, and TPH1 was associated with anticholinergic symptoms in a generalized linear univariate model, with body mass index, clozapine monotherapy, and GRS as explaining variables (permuted P = 0.014).

3. Cristofaro I., et al. Activation of M2 muscarinic acetylcholine receptors by a hybrid agonist enhances cytotoxic effects in GB7 glioblastoma cancer stem cells. Neurochemistry International. 2018, 118: 52-60. PubMed ID: 29702145
   
   

   The researcher implicates that N-8-Iper is an M2 activator which produces a cytotoxic and promotes the cell apoptosis at low concentrations. These also suggest that M2 activator may be a promising therapeutic agent for glioblastoma cancer treatment.

4. Miyauchi M., et al. Association of the cholinergic muscarinic M2 receptor with autonomic nervous system activity in patients with schizophrenia on high-dose antipsychotics. Neuropsychobiology. 2016, 74(1): 60-67. PubMed ID: 27923235
   
   

   The article investigates the association between SNPs in CHRM1, CHRM2 and CHRM3 and autonomic nervous system (ANS) activity. The results show that the CHRM2 rs8191992 polymorphism in patients with schizophrenia on high-dose antipsychotics decreases ANS activity.

5. Cherubini E., et al. Genetic polymorphism of CHRM2 in COPD: clinical significance and therapeutic implications. Journal of Cellular Physiology. 2016, 231(8): 1745-1751. PubMed ID: 26633752
   
   

   The study identifies that the CHRM2 rs1824024 polymorphism is significantly associated with the severity of chronic obstructive pulmonary disease and it decreases lung function test values, gives rise to frequent exacerbations, and is a poor response to anticholinergic drugs.

CHRM2 Preparation Options

To obtain the soluble and functional target protein, the versatile Magic™ membrane protein production platform in Creative Biolabs enables many flexible options, from which you can always find a better match for your particular project. Aided by our versatile Magic™ anti-membrane protein antibody discovery platform, we also provide customized anti-CHRM2 antibody development services.

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