Property Summary

NCBI Gene PubMed Count 146
Grant Count 48
R01 Count 22
Funding $10,858,726.33
PubMed Score 429.68
PubTator Score 425.83

Knowledge Summary

Patent (11,135)

TINX Plot

  Disease Relevance (82)

Disease Z-score Confidence
Nephrolithiasis 30 5.058 2.5
Pain agnosia 99 3.715 1.9
Urinary tract obstruction 2 3.645 1.8
Pyelonephritis 12 3.54 1.8
Cholinergic urticaria 5 3.26 1.6
Ascending cholangitis 4 3.259 1.6
Acute cystitis 37 3.054 1.5
Urofacial syndrome 7 3.004 1.5
Allergic rhinitis 91
Aptyalism 1
Ascites 2
Asthma 349
Biliary dyskinesia 7
Bladder muscle dysfunction - overactive 4
Bronchitis 44
Bronchospasm 9
Bronchospasm Prevention with COPD 3
Cholinesterase Inhibitors Toxicity 4
Chronic Obstructive Pulmonary Disease wi... 8 
Chronic bronchitis 4
Chronic gastritis 5
Chronic obstructive lung disease 6
Common cold 63
Cough 21
Cryptorchidism 67
Cycloplegia 13
Diagnostic Test for Asthma 1
Dilated pupil 6
Drug-Induced Liver Injury 118
Dysuria 24
Enterocolitis 4
Epilepsy 346 2.0
Excessive salivation 5
Gastric ulcer 34
Gastrointestinal Radiography Adjunct 11
General anesthesia 53
Increased Urinary Frequency 11
Irritable bowel syndrome 59
Liver Cirrhosis 101
Muscarine Toxicity 3
Nasal congestion 24
Nasal discharge 26
Neurogenic bladder 16
Ocular hypertension 27
Open-angle glaucoma 26
Parkinson's disease 364
Peptic ulcer 22
Perioperative Mydriasis 3
Pick disease 1,893
Primary Closed Angle Glaucoma 1
Prune Belly Syndrome 1
Pulmonary emphysema 34
Retention of urine 3
Sinus bradycardia 3
Urethral obstruction sequence 1
Urge incontinence of urine 3
Urgent desire to urinate 11
Urinary Bladder Diseases 5
Urinary Tract Irritation 24
Urinary incontinence 13
Vagal Reflex Bradycardia 5
Vasomotor rhinitis 15
Xerostomia Secondary to Radiation Therap... 1 
Xerostomia Secondary to Sjogren's Syndro... 2 
active Crohn's disease 918
active ulcerative colitis 477
astrocytic glioma 2,241
atypical teratoid / rhabdoid tumor 4,369
chronic rhinosinusitis 512
cystic fibrosis 1,665
ependymoma 2,514
glioblastoma 5,572
group 4 medulloblastoma 1,875
intraductal papillary-mucinous neoplasm ... 3,289 
lung adenocarcinoma 2,713
oligodendroglioma 2,849
osteosarcoma 7,933
ovarian cancer 8,484
pancreatic cancer 2,300
pediatric high grade glioma 2,712
primary pancreatic ductal adenocarcinoma 1,271
psoriasis 6,685

Expression

  Differential Expression (20)

Disease log2 FC p
astrocytic glioma -3.800 0.002
ependymoma -4.600 0.000
oligodendroglioma -3.400 0.010
psoriasis -1.500 0.001
glioblastoma -3.500 0.002
osteosarcoma -1.728 0.022
atypical teratoid / rhabdoid tumor -4.000 0.000
primary pancreatic ductal adenocarcinoma -1.753 0.002
intraductal papillary-mucinous neoplasm ... -2.800 0.029
active Crohn's disease 2.897 0.006
active ulcerative colitis 1.691 0.024
Parkinson's disease -1.100 0.012
cystic fibrosis -1.800 0.000
pediatric high grade glioma -2.700 0.005
group 4 medulloblastoma 3.400 0.005
lung adenocarcinoma -1.100 0.000
Pick disease -1.500 0.047
ovarian cancer -1.400 0.020
chronic rhinosinusitis 1.078 0.050
pancreatic cancer -1.700 0.002

MLP Assay (13)

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
623926 confirmatory 0 / 0 / 10 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 (hM3 CounterScreen)
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)
743249 screening 1 / 0 / 0 Development of the First Potent, Selective and CNS penetrant M5 Negative Allosteric Modulator (NAM)
743250 screening 1 / 0 / 0 Discovery and characterization of a small molecule allosteric agonists of mas-related G-Protein coupled receptor X1 ( MrgX1)
743251 screening 1 / 0 / 0 Development of a novel orthosteric Muscarinic 5 (M5) antagonist possessing a hig degree of muscarinic subtype selectivity
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Gene RIF (111)

PMID Text
26956674 These findings indicate that M3 mAChR may be important therapeutic target for obstructive airway diseases, as it regulates the effects of the epithelial-derived chemokines on ASM cell migration, which results in lung remodeling.
26901532 results suggest that the autoantibodies against peptides of the second extracellular loop of M3R are not pathogenic in vivo and they are not suitable as biomarkers for pSS diagnosis
26692031 Report using biosensing techniques to monitor dynamic changes of inositol lipid pools in living cells reveals a PKC-dependent PtdIns4P increase upon EGF and M3 receptor activation.
26071486 Blockading CHRM3 by shRNA or treatment with darifenacin inhibited prostate cancer growth.
26066647 M3 AChR or AMP-activated protein kinase Small Interfering RNA abrogated the ACh-elicited the attenuation of Endoplasmic reticulum stress in endothelial cells, indicating that the salutary effects of ACh were likely mediated by M3 AChR-AMPK signaling.
25964092 ACh-induced activation of EGFR/PI3K/AKT pathway and subsequent IL-8 upregulation may be one of the important mechanisms of M3R function
25916507 Suggest Gbeta4gamma1 as a modulator of M3 muscarinic receptor signaling.
25769304 an incorrect organizational structure of many mutants of hM3R provides the molecular basis for why they are poorly expressed and fail to be effectively trafficked to the cell surface.
25375131 Cigarette smoking may contribute to this imbalance by affecting the polarization and survival of Th/Tregs through the up-regulation of MR3 and MR5.
25316767 Results uncovered that Gaq binding to GRK2 enhances the recruitment of GRK2 to M3-ACh receptors.
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AA Sequence

MTLHNNSTTSPLFPNISSSWIHSPSDAGLPPGTVTHFGSYNVSRAAGNFSSPDGTTDDPLGGHTVWQVVF      1 - 70
IAFLTGILALVTIIGNILVIVSFKVNKQLKTVNNYFLLSLACADLIIGVISMNLFTTYIIMNRWALGNLA     71 - 140
CDLWLAIDYVASNASVMNLLVISFDRYFSITRPLTYRAKRTTKRAGVMIGLAWVISFVLWAPAILFWQYF    141 - 210
VGKRTVPPGECFIQFLSEPTITFGTAIAAFYMPVTIMTILYWRIYKETEKRTKELAGLQASGTEAETENF    211 - 280
VHPTGSSRSCSSYELQQQSMKRSNRRKYGRCHFWFTTKSWKPSSEQMDQDHSSSDSWNNNDAAASLENSA    281 - 350
SSDEEDIGSETRAIYSIVLKLPGHSTILNSTKLPSSDNLQVPEEELGMVDLERKADKLQAQKSVDDGGSF    351 - 420
PKSFSKLPIQLESAVDTAKTSDVNSSVGKSTATLPLSFKEATLAKRFALKTRSQITKRKRMSLVKEKKAA    421 - 490
QTLSAILLAFIITWTPYNIMVLVNTFCDSCIPKTFWNLGYWLCYINSTVNPVCYALCNKTFRTTFKMLLL    491 - 560
CQCDKKKRRKQQYQQRQSVIFHKRAPEQAL                                            561 - 590
//

Text Mined References (148)

PMID Year Title
26956674 2016 The activation of M3 mAChR in airway epithelial cells promotes IL-8 and TGF-?1 secretion and airway smooth muscle cell migration.
26901532 2016 Autoantibodies against the Second Extracellular Loop of M3R Do neither Induce nor Indicate Primary Sjögren's Syndrome.
26692031 2016 BRET-monitoring of the dynamic changes of inositol lipid pools in living cells reveals a PKC-dependent PtdIns4P increase upon EGF and M3 receptor activation.
26071486 2015 Autocrine Activation of CHRM3 Promotes Prostate Cancer Growth and Castration Resistance via CaM/CaMKK-Mediated Phosphorylation of Akt.
26066647 2015 Acetylcholine ameliorates endoplasmic reticulum stress in endothelial cells after hypoxia/reoxygenation via M3 AChR-AMPK signaling.
25964092 2015 Activation of M3 muscarinic receptor by acetylcholine promotes non-small cell lung cancer cell proliferation and invasion via EGFR/PI3K/AKT pathway.
25916507 2015 G?4?1 as a modulator of M3 muscarinic receptor signalling and novel roles of G?1 subunits in the modulation of cellular signalling.
25769304 2015 The molecular basis of oligomeric organization of the human M3 muscarinic acetylcholine receptor.
25375131 2014 Cigarette smoking promotes inflammation in patients with COPD by affecting the polarization and survival of Th/Tregs through up-regulation of muscarinic receptor 3 and 5 expression.
25316767 2015 Influence of g?q on the dynamics of m3-acetylcholine receptor-g-protein-coupled receptor kinase 2 interaction.
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