Muscarinic acetylcholine receptor M2
Details
- Name
- Muscarinic acetylcholine receptor M2
- Kind
- protein
- Synonyms
- Not Available
- Gene Name
- CHRM2
- UniProtKB Entry
- P08172Swiss-Prot
- Organism
- Humans
- NCBI Taxonomy ID
- 9606
- Amino acid sequence
>lcl|BSEQ0016133|Muscarinic acetylcholine receptor M2 MNNSTNSSNNSLALTSPYKTFEVVFIVLVAGSLSLVTIIGNILVMVSIKVNRHLQTVNNY FLFSLACADLIIGVFSMNLYTLYTVIGYWPLGPVVCDLWLALDYVVSNASVMNLLIISFD RYFCVTKPLTYPVKRTTKMAGMMIAAAWVLSFILWAPAILFWQFIVGVRTVEDGECYIQF FSNAAVTFGTAIAAFYLPVIIMTVLYWHISRASKSRIKKDKKEPVANQDPVSPSLVQGRI VKPNNNNMPSSDDGLEHNKIQNGKAPRDPVTENCVQGEEKESSNDSTSVSAVASNMRDDE ITQDENTVSTSLGHSKDENSKQTCIRIGTKTPKSDSCTPTNTTVEVVGSSGQNGDEKQNI VARKIVKMTKQPAKKKPPPSREKKVTRTILAILLAFIITWAPYNVMVLINTFCAPCIPNT VWTIGYWLCYINSTINPACYALCNATFKKTFKHLLMCHYKNIGATR
- Number of residues
- 466
- Molecular Weight
- 51714.605
- Theoretical pI
- 9.08
- GO Classification
- Functionsarrestin family protein binding / G protein-coupled acetylcholine receptor activity / G protein-coupled serotonin receptor activityProcessesadenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathway / adenylate cyclase-modulating G protein-coupled receptor signaling pathway / chemical synaptic transmission / G protein-coupled acetylcholine receptor signaling pathway / G protein-coupled receptor signaling pathway / G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger / phospholipase C-activating G protein-coupled acetylcholine receptor signaling pathway / presynaptic modulation of chemical synaptic transmissionComponentscholinergic synapse / clathrin-coated endocytic vesicle membrane / glutamatergic synapse / membrane / presynaptic membrane
- General Function
- The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the action of G proteins. Primary transducing effect is adenylate cyclase inhibition. Signaling promotes phospholipase C activity, leading to the release of inositol trisphosphate (IP3); this then triggers calcium ion release into the cytosol
- Specific Function
- arrestin family protein binding
- Pfam Domain Function
- 7tm_1 (PF00001)
- Signal Regions
- Not Available
- Transmembrane Regions
- 23-45 60-80 98-119 140-162 185-209 388-410 419-442
- Cellular Location
- Cell membrane
- Gene sequence
>lcl|BSEQ0016134|Muscarinic acetylcholine receptor M2 (CHRM2) ATGAATAACTCAACAAACTCCTCTAACAATAGCCTGGCTCTTACAAGTCCTTATAAGACA TTTGAAGTGGTGTTTATTGTCCTGGTGGCTGGATCCCTCAGTTTGGTGACCATTATCGGG AACATCCTAGTCATGGTTTCCATTAAAGTCAACCGCCACCTCCAGACCGTCAACAATTAC TTTTTATTCAGCTTGGCCTGTGCTGACCTTATCATAGGTGTTTTCTCCATGAACTTGTAC ACCCTCTACACTGTGATTGGTTACTGGCCTTTGGGACCTGTGGTGTGTGACCTTTGGCTA GCCCTGGACTATGTGGTCAGCAATGCCTCAGTTATGAATCTGCTCATCATCAGCTTTGAC AGGTACTTCTGTGTCACAAAACCTCTGACCTACCCAGTCAAGCGGACCACAAAAATGGCA GGTATGATGATTGCAGCTGCCTGGGTCCTCTCTTTCATCCTCTGGGCTCCAGCCATTCTC TTCTGGCAGTTCATTGTAGGGGTGAGAACTGTGGAGGATGGGGAGTGCTACATTCAGTTT TTTTCCAATGCTGCTGTCACCTTTGGTACGGCTATTGCAGCCTTCTATTTGCCAGTGATC ATCATGACTGTGCTATATTGGCACATATCCCGAGCCAGCAAGAGCAGGATAAAGAAGGAC AAGAAGGAGCCTGTTGCCAACCAAGACCCCGTTTCTCCAAGTCTGGTACAAGGAAGGATA GTGAAGCCAAACAATAACAACATGCCCAGCAGTGACGATGGCCTGGAGCACAACAAAATC CAGAATGGCAAAGCCCCCAGGGATCCTGTGACTGAAAACTGTGTTCAGGGAGAGGAGAAG GAGAGCTCCAATGACTCCACCTCAGTCAGTGCTGTTGCCTCTAATATGAGAGATGATGAA ATAACCCAGGATGAAAACACAGTTTCCACTTCCCTGGGCCATTCCAAAGATGAGAACTCT AAGCAAACATGCATCAGAATTGGCACCAAGACCCCAAAAAGTGACTCATGTACCCCAACT AATACCACCGTGGAGGTAGTGGGGTCTTCAGGTCAGAATGGAGATGAAAAGCAGAATATT GTAGCCCGCAAGATTGTGAAGATGACTAAGCAGCCTGCAAAAAAGAAGCCTCCTCCTTCC CGGGAAAAGAAAGTCACCAGGACAATCTTGGCTATTCTGTTGGCTTTCATCATCACTTGG GCCCCATACAATGTCATGGTGCTCATTAACACCTTTTGTGCACCTTGCATCCCCAACACT GTGTGGACAATTGGTTACTGGCTTTGTTACATCAACAGCACTATCAACCCTGCCTGCTAT GCACTTTGCAATGCCACCTTCAAGAAGACCTTTAAACACCTTCTCATGTGTCATTATAAG AACATAGGCGCTACAAGGTAA
- Chromosome Location
- 7
- Locus
- 7q33
- External Identifiers
Resource Link UniProtKB ID P08172 UniProtKB Entry Name ACM2_HUMAN GenBank Protein ID 177990 GenBank Gene ID M16404 GeneCard ID CHRM2 GenAtlas ID CHRM2 HGNC ID HGNC:1951 PDB ID(s) 3UON, 4MQS, 4MQT, 5YC8, 5ZK3, 5ZK8, 5ZKB, 5ZKC, 6OIK, 6U1N, 7T8X, 7T90, 7T94, 7T96, 8J8R, 8J97, 8JAF KEGG ID hsa:1129 IUPHAR/Guide To Pharmacology ID 14 NCBI Gene ID 1129 - General References
- Bonner TI, Buckley NJ, Young AC, Brann MR: Identification of a family of muscarinic acetylcholine receptor genes. Science. 1987 Jul 31;237(4814):527-32. [Article]
- Peralta EG, Ashkenazi A, Winslow JW, Smith DH, Ramachandran J, Capon DJ: Distinct primary structures, ligand-binding properties and tissue-specific expression of four human muscarinic acetylcholine receptors. EMBO J. 1987 Dec 20;6(13):3923-9. [Article]
- Gerhard DS, Wagner L, Feingold EA, Shenmen CM, Grouse LH, Schuler G, Klein SL, Old S, Rasooly R, Good P, Guyer M, Peck AM, Derge JG, Lipman D, Collins FS, Jang W, Sherry S, Feolo M, Misquitta L, Lee E, Rotmistrovsky K, Greenhut SF, Schaefer CF, Buetow K, Bonner TI, Haussler D, Kent J, Kiekhaus M, Furey T, Brent M, Prange C, Schreiber K, Shapiro N, Bhat NK, Hopkins RF, Hsie F, Driscoll T, Soares MB, Casavant TL, Scheetz TE, Brown-stein MJ, Usdin TB, Toshiyuki S, Carninci P, Piao Y, Dudekula DB, Ko MS, Kawakami K, Suzuki Y, Sugano S, Gruber CE, Smith MR, Simmons B, Moore T, Waterman R, Johnson SL, Ruan Y, Wei CL, Mathavan S, Gunaratne PH, Wu J, Garcia AM, Hulyk SW, Fuh E, Yuan Y, Sneed A, Kowis C, Hodgson A, Muzny DM, McPherson J, Gibbs RA, Fahey J, Helton E, Ketteman M, Madan A, Rodrigues S, Sanchez A, Whiting M, Madari A, Young AC, Wetherby KD, Granite SJ, Kwong PN, Brinkley CP, Pearson RL, Bouffard GG, Blakesly RW, Green ED, Dickson MC, Rodriguez AC, Grimwood J, Schmutz J, Myers RM, Butterfield YS, Griffith M, Griffith OL, Krzywinski MI, Liao N, Morin R, Palmquist D, Petrescu AS, Skalska U, Smailus DE, Stott JM, Schnerch A, Schein JE, Jones SJ, Holt RA, Baross A, Marra MA, Clifton S, Makowski KA, Bosak S, Malek J: The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC). Genome Res. 2004 Oct;14(10B):2121-7. [Article]
- Kitano T, Liu YH, Ueda S, Saitou N: Human-specific amino acid changes found in 103 protein-coding genes. Mol Biol Evol. 2004 May;21(5):936-44. Epub 2004 Mar 10. [Article]
- Gurevich VV, Dion SB, Onorato JJ, Ptasienski J, Kim CM, Sterne-Marr R, Hosey MM, Benovic JL: Arrestin interactions with G protein-coupled receptors. Direct binding studies of wild type and mutant arrestins with rhodopsin, beta 2-adrenergic, and m2 muscarinic cholinergic receptors. J Biol Chem. 1995 Jan 13;270(2):720-31. [Article]
- Leong WF, Chow VT: Transcriptomic and proteomic analyses of rhabdomyosarcoma cells reveal differential cellular gene expression in response to enterovirus 71 infection. Cell Microbiol. 2006 Apr;8(4):565-80. [Article]
- Wang JC, Hinrichs AL, Stock H, Budde J, Allen R, Bertelsen S, Kwon JM, Wu W, Dick DM, Rice J, Jones K, Nurnberger JI Jr, Tischfield J, Porjesz B, Edenberg HJ, Hesselbrock V, Crowe R, Schuckit M, Begleiter H, Reich T, Goate AM, Bierut LJ: Evidence of common and specific genetic effects: association of the muscarinic acetylcholine receptor M2 (CHRM2) gene with alcohol dependence and major depressive syndrome. Hum Mol Genet. 2004 Sep 1;13(17):1903-11. Epub 2004 Jun 30. [Article]
- Reiner CL, McCullar JS, Kow RL, Le JH, Goodlett DR, Nathanson NM: RACK1 associates with muscarinic receptors and regulates M(2) receptor trafficking. PLoS One. 2010 Oct 20;5(10):e13517. doi: 10.1371/journal.pone.0013517. [Article]
- Haga K, Kruse AC, Asada H, Yurugi-Kobayashi T, Shiroishi M, Zhang C, Weis WI, Okada T, Kobilka BK, Haga T, Kobayashi T: Structure of the human M2 muscarinic acetylcholine receptor bound to an antagonist. Nature. 2012 Jan 25;482(7386):547-51. doi: 10.1038/nature10753. [Article]
- Kruse AC, Ring AM, Manglik A, Hu J, Hu K, Eitel K, Hubner H, Pardon E, Valant C, Sexton PM, Christopoulos A, Felder CC, Gmeiner P, Steyaert J, Weis WI, Garcia KC, Wess J, Kobilka BK: Activation and allosteric modulation of a muscarinic acetylcholine receptor. Nature. 2013 Dec 5;504(7478):101-6. doi: 10.1038/nature12735. Epub 2013 Nov 20. [Article]
Associated Data
- Drug Relations
Drug Drug group Pharmacological action? Type Actions Details Atropine approved, vet_approved yes target antagonist Details Homatropine methylbromide approved yes target antagonist Details Cryptenamine approved yes target antagonist Details Diphenidol approved, investigational, withdrawn yes target antagonist Details Ipratropium approved, experimental yes target antagonist Details Olanzapine approved, investigational unknown target antagonist Details Oxyphencyclimine approved yes target antagonist Details Procyclidine approved yes target antagonist Details Carbamoylcholine approved yes target agonist Details Hyoscyamine approved yes target antagonist Details Gallamine triethiodide approved yes target antagonist Details Tridihexethyl withdrawn yes target antagonist Details Triflupromazine approved, vet_approved yes target antagonist Details Anisotropine methylbromide approved yes target antagonist Details Rocuronium approved yes target antagonist Details Benzquinamide withdrawn yes target antagonist Details Tolterodine approved, investigational yes target antagonist Details Promethazine approved, investigational unknown target antagonist Details Doxacurium approved unknown target antagonist Details Flavoxate approved yes target antagonist Details Desipramine approved, investigational no target antagonist Details Mivacurium approved no target antagonistpartial agonist Details Methotrimeprazine approved, investigational unknown target antagonist Details Oxybutynin approved, investigational yes target antagonist Details Pilocarpine approved, investigational yes target agonist Details Metocurine approved unknown target antagonist Details ALKS 27 investigational unknown target Details Nicardipine approved, investigational unknown target antagonist Details Quetiapine approved unknown target ligand Details Tiotropium approved unknown target antagonist Details Ziprasidone approved unknown target antagonist Details Clozapine approved unknown target partial agonist Details Darifenacin approved, investigational unknown target antagonist Details Cocaine approved, illicit unknown target antagonist Details Pipecuronium approved unknown target antagonist Details Pancuronium approved unknown target antagonist Details Disopyramide approved unknown target antagonist Details Profenamine approved unknown target antagonist Details Chlorprothixene approved, experimental, investigational, withdrawn no target antagonist Details Doxepin approved, investigational unknown target antagonist Details Imipramine approved no target antagonist Details Cyproheptadine approved unknown target antagonist Details Brompheniramine approved unknown target antagonist Details Tropicamide approved, investigational yes target antagonist Details Dicyclomine approved unknown target antagonist Details Scopolamine approved, investigational yes target antagonist Details Trihexyphenidyl approved unknown target antagonist Details Solifenacin approved unknown target antagonist Details Succinylcholine approved unknown target agonist Details Maprotiline approved, investigational no target antagonist Details Methscopolamine bromide approved yes target antagonist Details Dimetindene approved, investigational yes target antagonist Details Fesoterodine approved unknown target antagonist Details Bethanechol approved unknown target agonist Details Aclidinium approved yes target antagonist Details Loxapine approved unknown target binder Details Terfenadine approved, withdrawn unknown target binder Details Glycopyrronium approved, investigational, vet_approved yes target antagonist Details Umeclidinium approved unknown target antagonist Details Diphenhydramine approved, investigational unknown target antagonist Details Hexocyclium approved unknown target antagonist Details Butylscopolamine approved, investigational, vet_approved unknown target antagonist Details Dosulepin approved yes target antagonist Details Imidafenacin investigational yes target antagonist Details Acetylcholine approved, investigational unknown target Details Homatropine approved yes target antagonist Details Pizotifen approved unknown target antagonist Details Propiverine approved, investigational yes target antagonist Details Thonzylamine approved unknown target antagonist Details Rapacuronium approved, withdrawn yes target antagonist Details Rociverine experimental yes target antagonist Details Trimebutine approved yes target antagonist Details Aripiprazole lauroxil approved, investigational no target Details Aripiprazole approved, investigational unknown target ligand Details Methantheline approved, investigational unknown target Details Methacholine approved, investigational yes target agonist Details Viloxazine approved, investigational, withdrawn unknown target antagonist Details Cisatracurium approved, investigational unknown target antagonist Details Caramiphen experimental, vet_approved yes target inhibitor Details Methscopolamine approved yes target antagonist Details Aceclidine approved yes target inhibitor Details