Recombinant Human Muscarinic acetylcholine receptor M2 (CHRM2)

1. A key step in CHRM2 activation is the exchange of a Na+ ion from an extracellular binding pocket to the cytoplasm. PMID: 29249607
2. Ligation of the identical phosphopeptide onto the beta2AR, the muscarinic acetylcholine receptor 2 and the mu-opioid receptor reveals that the ability of beta-arrestin1 to enhance agonist binding relative to G protein differs substantially among receptors. PMID: 29581292
3. Data suggests that RBM24 binds to coding region of CHRM2 to regulate mRNA stability in cardiomyocytes; RBM24appears to drive changes in alternative splicing and in production of alternative transcript isoforms. (RBM24 = RNA binding motif protein-24; CHRM2 = cholinergic receptor muscarinic 2) PMID: 29104163
4. T allele carrying status (GT and TT) [rs1824024] of muscarinic cholinergic receptor 2 (CHRM2) may be associated with delirium tremens. PMID: 29478862
5. Two single nucleotide polymorphisms in CHRM2 gene, rs2061174 and rs6948054, showed significant difference in genotype distribution between medical and fine arts students (p<0.05). The rs2061174 showed significant at p = 0.001, OR and 95% CI were 3.78 (2.00-7.14), whereas the rs6948054 was significant at p = 0.012, OR and 95% CI were 2.50 (1.32-4.77). PMID: 29906045
6. complex between M2R and holo-Gi1 is an octamer comprising four copies of each, and that activation is accompanied by a decrease in the oligomeric size of Gi1 PMID: 27494760
7. Graded activation and free energy landscapes of a muscarinic G-protein-coupled M2 receptor has been reported. PMID: 27791003
8. With final functional experiments on six selected compounds, we confirmed four of them as new negative allosteric modulators (NAMs) and one as positive allosteric modulator of agonist-mediated response at the M2 mAChR PMID: 27601651
9. Results show reduced autonomic nervous system (ANS) activity in association with the CHRM2 rs8191992 polymorphism in patients with schizophrenia on high-dose antipsychotics. CHRM2 polymorphisms may play an important role in ANS activity in patients with schizophrenia. PMID: 27923235
10. Data suggest that levels of CHRM2 are lower in Brodmann's area 24 from subjects with mood disorders, and it is possible that signalling by that receptor is also less in this cortical region; increasing levels of CHRM2 may be involved in the mechanisms of action of mood stabilisers and tricyclic antidepressants PMID: 26475745
11. These results suggest that the M2 receptors may represent a new interesting therapeutic tool to counteract glioblastoma cancer stem cell growth and survival. PMID: 26033491
12. Report a significant association between CHRM2 (rs1824024) polymorphism and disease severity, lower lung function test values, frequent exacerbations, and poor response to anti-cholinergic drugs in COPD patients. PMID: 26633752
13. Inactivation of M2 AChR/NF-kappaB signaling axis reverses epithelial-mesenchymal transition and suppresses migration and invasion in non-small cell lung cancer. PMID: 26336823
14. CHRM2 gene expression was dysregulated in the anterior cingulate of bipolar patients. PMID: 26238605
15. Higher serum anti-M2-R and anti-beta1-R levels are associated with lone paroxysmal atrial fibrillation. PMID: 25351416
16. This study demonstrated that CD4+ and CD8+ T cells expressed M2 and M4 muscarinic receptors which density were significantly increased in asthmatic children in comparison with controls. PMID: 26025056
17. The expressed the fusion proteins of the muscarinic acetylcholine receptor M2 subtype with a maltose-binding protein and various G protein alpha subunits in Escherichia coli. PMID: 24881046
18. High Muscarinic Receptor M2 expression is associated with peripartum cardiomyopathy. PMID: 24466231
19. It was the M(2) receptor pharmacology. PMID: 24807965
20. [(3)H]LY2119620 to probe specifically the human M2 and M4 muscarinic receptor allosteric binding sites. PMID: 24807966
21. The present report found an association between genetic variation of the CHRM2 rs1824024 SNP in the 8-12 year old group and not in the older age groups. PMID: 23747232
22. This novel study demonstrated for the first time a full-scale screening of the proteomics research by CHRM2-C722G mutation and profiled 102 changed proteins, of which, eight might be critical in cardiac dysfunction PMID: 23743182
23. Activation occurs by formation of a Tyr206-Tyr440 hydrogen bond and 6A outward tilting of the cytoplasmic end of transmembrane alpha-helix 6, preceded by relocation of Trp400 toward Phe195 and Val199 and flipping of Tyr430 away from the ligand-binding cavity. PMID: 23781107
24. Muscarinic M2 receptor stimulation enhances TGF-beta1-induced airway smooth muscle cell proliferation. PMID: 23449734
25. The allosteric vestibule of CHRM2 controls G-protein coupling. PMID: 22948826
26. These data suggest a role for M2 muscarinic receptors in the inhibition of glioma cell proliferation and the possibility of exploiting these receptors as new promising tools for glioblastoma therapy. PMID: 22575825
27. Mutations in an allosteric binding pocket in the M2 muscarinic acetylcholine receptor introduces stimulus bias in response to atypical ligands. PMID: 22965232
28. Exposure to the cholinergic agonist carbachol induced a concentration-dependent increase in cell proliferation rate. This effect was mainly mediated by the receptor subtypes M3 and M2. PMID: 22610841
29. Identification of functionally active autoantibodies to CHRM2 in serum samples from complex regional pain syndrome (CRPS) patients supports an autoimmune pathogenesis of CRPS. PMID: 21816540
30. Findings indicate that relative to a normative "lower risk" externalizing trajectory, likelihood of membership in two "higher risk" trajectories increased with each additional copy of the minor allelic variant at CHRM2. PMID: 21883161
31. Xray structure of the antagonist-bound human M2 receptor, the first human acetylcholine receptor to be characterized structurally PMID: 22278061
32. Influenza infection significantly increased TNF-alpha release from isolated epithelial cells, sufficient to decrease M receptors in neuroblastoma cells. PMID: 21457223
33. SNP rs1455858 associated with adolescent substance abuse and temperamental risk factors PMID: 21494862
34. association of SNPs with adolescent externalizing behavior and relation to parental monitoring PMID: 21441226
35. one SNP (with identifier rs324650, in which the ancestral allele adenine (A) is replaced with one or two copies of thymine (T), showed a significant allelic effect on V(T) in the pregenual and subgenual anterior cingulate cortices in the direction AA PMID: 20351719
36. muscarinic acetylcholine function might be related not with alcohol dependence itself but with the severity of alcohol dependence in Korean population PMID: 21176104
37. a variant in the muscarinic acetylcholine receptor 2 gene (CHRM2) may have a role in nicotine addiction PMID: 19644963
38. Distribution of M2 receptors in human colon. PMID: 20146726
39. analysis of the oligomeric size of the m2 muscarinic receptor in live cells PMID: 20304928
40. Data suggest that the functional selectivity of the M2 muscarinic receptor for such agents may arise from a bitopic mechanism. PMID: 20051519
41. trafficking of M2 muscarinic acetylcholine receptor to clathrin-derived early endosomes following clathrin-independent endocytosis PMID: 12093817
42. Results are consistent with a gender-specific role of the CHRM2 gene in depression in women. PMID: 12116189
43. There is a higher concentration of muscarinic-2 receptors in the brain of aging subjects with an apolipoprotein E-epsilon4 allele. PMID: 12774299
44. molecular model of orthosteric and allosteric binding sites PMID: 12825791
45. Data characterize the 5' untranslated region of the CHRM2 gene as expressed in human airway smooth muscle (HASM) cells. PMID: 14512373
46. Whereas normal detrusor contractions are mediated by the M(3) receptor subtype, in patients with neurogenic bladder dysfunction as well as certain organ transplant donors, contractions can be mediated by the M(2) muscarinic receptor subtype. PMID: 14751843
47. Linkage and linkage disequilibrium between frontal theta band, visual evoked brain potentials and single nucleotide polymorphism(SNP) from CHRM2 on chromosome 7. Linkage disequilibrium between CHRM2 SNPs and parietal delta band visual evoked potentials. PMID: 15210286
48. Extracts of M2 muscarinic receptor from Sf9 cells therefore contain aggregates that are at least trimeric, and the levels detected point to the existence of larger complexes. The data also suggest that the oligomers coexist with a population of monomers PMID: 15255931
49. variations in the CHRM2 gene is associated with alcohol dependence, drug dependence and affective disorders PMID: 16000316
50. M2 acetylcholine receptor down-regulation in brains with Alzheimer's disease(AD) affects expression of several genes and proteins with major functions in the pathology of AD, including beta-secretase BACE1 and several modulators of tau protein. PMID: 16181410

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HGNC: 1951

OMIM: 103780

KEGG: hsa:1129

STRING: 9606.ENSP00000319984

UniGene: Hs.535891