Property Summary

NCBI Gene PubMed Count 128
Grant Count 20
R01 Count 6
Funding $2,351,143.49
PubMed Score 489.71
PubTator Score 285.74

Knowledge Summary

Patent (6,250)

Expression

  Differential Expression (3)

Disease log2 FC p
medulloblastoma, large-cell 1.200 0.000
colon cancer -3.000 0.000
psoriasis -2.300 0.000

 GWAS Trait (1)

MLP Assay (18)

AID Type Active / Inconclusive / Inactive Description
1788 other 0 / 0 / 0 Discovery of novel allosteric modulators of the M1 muscarinic receptor: Agonist Ancillary Activity
1921 other 2 / 0 / 0 Discovery of a Highly Selective in vitro and in vivo M4 Positive Allosteric Modulator: Ancillary Activity
588746 confirmatory 1 / 0 / 8 Human M2 PAM Extended Characterization CounterScreen (CRC)
623925 confirmatory 1 / 0 / 9 Chemical optimization of in vitro pharmacology and DMPK properties of the highly selective mAChR 4 (M4) Positive Allosteric Modulator (PAM) Series with Greatly Improved Human Receptor Activity (hM2 CounterScreen)
651924 confirmatory 0 / 0 / 1 Discovery of Selective Novel Positive Allosteric Modulators (PAM) of the Muscarinic Receptor (M5) in CHO cells expressing human M2 receptor
686924 other 0 / 0 / 1 ML347 Eurofin Panel Assay for BMP Inhibitor (Probe Compound)
686925 other 0 / 0 / 1 ML352 Eurofin Panel Assay for Choline Transporter Inhibitor (Probe Compound)
686926 other 0 / 0 / 1 ML354 Eurofin Panel Assay for PAR4 Antagonists Inhibitor (Probe Compound)
686927 other 0 / 0 / 1 ML353 Eurofin Panel Assay for mGlu5 SAM Inhibitor (Probe Compound)
743096 confirmatory 0 / 0 / 6 Discovery of Novel Positive Allosteric Modulators (PAMs) of Muscarinic Receptor M5: Counterscreen against human M2
More...

Gene RIF (104)

PMID Text
26633752 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.
26336823 Inactivation of M2 AChR/NF-kappaB signaling axis reverses epithelial-mesenchymal transition and suppresses migration and invasion in non-small cell lung cancer.
26238605 CHRM2 gene expression was dysregulated in the anterior cingulate of bipolar patients.
26033491 These results suggest that the M2 receptors may represent a new interesting therapeutic tool to counteract glioblastoma cancer stem cell growth and survival.
26025056 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.
25351416 Higher serum anti-M2-R and anti-beta1-R levels are associated with lone paroxysmal atrial fibrillation.
24881046 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.
24807966 [(3)H]LY2119620 to probe specifically the human M2 and M4 muscarinic receptor allosteric binding sites.
24807965 It was the M(2) receptor pharmacology.
24466231 High Muscarinic Receptor M2 expression is associated with peripartum cardiomyopathy.
More...

AA Sequence

MNNSTNSSNNSLALTSPYKTFEVVFIVLVAGSLSLVTIIGNILVMVSIKVNRHLQTVNNYFLFSLACADL      1 - 70
IIGVFSMNLYTLYTVIGYWPLGPVVCDLWLALDYVVSNASVMNLLIISFDRYFCVTKPLTYPVKRTTKMA     71 - 140
GMMIAAAWVLSFILWAPAILFWQFIVGVRTVEDGECYIQFFSNAAVTFGTAIAAFYLPVIIMTVLYWHIS    141 - 210
RASKSRIKKDKKEPVANQDPVSPSLVQGRIVKPNNNNMPSSDDGLEHNKIQNGKAPRDPVTENCVQGEEK    211 - 280
ESSNDSTSVSAVASNMRDDEITQDENTVSTSLGHSKDENSKQTCIRIGTKTPKSDSCTPTNTTVEVVGSS    281 - 350
GQNGDEKQNIVARKIVKMTKQPAKKKPPPSREKKVTRTILAILLAFIITWAPYNVMVLINTFCAPCIPNT    351 - 420
VWTIGYWLCYINSTINPACYALCNATFKKTFKHLLMCHYKNIGATR                            421 - 466
//

Text Mined References (132)

PMID Year Title
26633752 2016 Genetic Polymorphism of CHRM2 in COPD: Clinical Significance and Therapeutic Implications.
26336823 2015 Inactivation of M2 AChR/NF-?B signaling axis reverses epithelial-mesenchymal transition (EMT) and suppresses migration and invasion in non-small cell lung cancer (NSCLC).
26238605 2015 Transcriptome sequencing of the anterior cingulate in bipolar disorder: dysregulation of G protein-coupled receptors.
26033491 2015 The activation of M2 muscarinic receptor inhibits cell growth and survival in human glioblastoma cancer stem cells.
26025056 2015 Modified expression of peripheral blood lymphocyte muscarinic cholinergic receptors in asthmatic children.
25351416 2015 Elevated M2-muscarinic and ?1-adrenergic receptor autoantibody levels are associated with paroxysmal atrial fibrillation.
24881046 2014 Interaction of the muscarinic acetylcholine receptor M? subtype with G protein G?(i/o) isotypes and G?? subunits as studied with the maltose-binding protein-M?-G?(i/o) fusion proteins expressed in Escherichia coli.
24807966 2014 Development of a radioligand, [(3)H]LY2119620, to probe the human M(2) and M(4) muscarinic receptor allosteric binding sites.
24807965 2014 Characterization of the novel positive allosteric modulator, LY2119620, at the muscarinic M(2) and M(4) receptors.
24466231 2014 The correlation between peripartum cardiomyopathy and autoantibodies against cardiovascular receptors.
More...