Adenosine receptor A2a

Details

Name
Adenosine receptor A2a
Synonyms
  • ADORA2
Gene Name
ADORA2A
Organism
Humans
Amino acid sequence
>lcl|BSEQ0001840|Adenosine receptor A2a
MPIMGSSVYITVELAIAVLAILGNVLVCWAVWLNSNLQNVTNYFVVSLAAADIAVGVLAI
PFAITISTGFCAACHGCLFIACFVLVLTQSSIFSLLAIAIDRYIAIRIPLRYNGLVTGTR
AKGIIAICWVLSFAIGLTPMLGWNNCGQPKEGKNHSQGCGEGQVACLFEDVVPMNYMVYF
NFFACVLVPLLLMLGVYLRIFLAARRQLKQMESQPLPGERARSTLQKEVHAAKSLAIIVG
LFALCWLPLHIINCFTFFCPDCSHAPLWLMYLAIVLSHTNSVVNPFIYAYRIREFRQTFR
KIIRSHVLRQQEPFKAAGTSARVLAAHGSDGEQVSLRLNGHPPGVWANGSAPHPERRPNG
YALGLVSGGSAQESQGNTGLPDVELLSHELKGVCPEPPGLDDPLAQDGAGVS
Number of residues
412
Molecular Weight
44706.925
Theoretical pI
8.05
GO Classification
Functions
enzyme binding / G-protein coupled adenosine receptor activity / identical protein binding
Processes
activation of adenylate cyclase activity / adenylate cyclase-modulating G-protein coupled receptor signaling pathway / apoptotic process / astrocyte activation / blood circulation / blood coagulation / cAMP biosynthetic process / cell-cell signaling / cellular defense response / cellular protein metabolic process / central nervous system development / eating behavior / excitatory postsynaptic potential / inflammatory response / inhibitory postsynaptic potential / locomotory behavior / membrane depolarization / negative regulation of alpha-beta T cell activation / negative regulation of cell proliferation / negative regulation of cysteine-type endopeptidase activity involved in apoptotic process / negative regulation of inflammatory response / negative regulation of locomotion / negative regulation of neuron apoptotic process / negative regulation of protein kinase activity / negative regulation of vascular permeability / neuron projection morphogenesis / neurotrophin TRK receptor signaling pathway / phagocytosis / positive regulation of acetylcholine secretion, neurotransmission / positive regulation of adenylate cyclase activity involved in G-protein coupled receptor signaling pathway / positive regulation of apoptotic signaling pathway / positive regulation of circadian sleep/wake cycle, sleep / positive regulation of glutamate secretion / positive regulation of protein secretion / positive regulation of renal sodium excretion / positive regulation of synaptic transmission, GABAergic / positive regulation of synaptic transmission, glutamatergic / positive regulation of urine volume / prepulse inhibition / protein kinase C-activating G-protein coupled receptor signaling pathway / regulation of calcium ion transport / regulation of mitochondrial membrane potential / regulation of norepinephrine secretion / regulation of synaptic plasticity / regulation of transcription, DNA-templated / response to amphetamine / response to caffeine / response to drug / sensory perception / synaptic transmission, cholinergic / synaptic transmission, dopaminergic / synaptic transmission, glutamatergic / transmembrane receptor protein tyrosine kinase signaling pathway / vasodilation
Components
asymmetric synapse / axolemma / dendrite / endomembrane system / integral component of plasma membrane / intermediate filament / membrane / neuronal cell body / plasma membrane / postsynaptic density / postsynaptic membrane / presynaptic active zone / presynaptic membrane
General Function
Identical protein binding
Specific Function
Receptor for adenosine. The activity of this receptor is mediated by G proteins which activate adenylyl cyclase.
Pfam Domain Function
Transmembrane Regions
8-32 43-66 78-100 121-143 174-198 235-258 267-290
Cellular Location
Cell membrane
Gene sequence
>lcl|BSEQ0016254|Adenosine receptor A2a (ADORA2A)
ATGCCCATCATGGGCTCCTCGGTGTACATCACGGTGGAGCTGGCCATTGCTGTGCTGGCC
ATCCTGGGCAATGTGCTGGTGTGCTGGGCCGTGTGGCTCAACAGCAACCTGCAGAACGTC
ACCAACTACTTTGTGGTGTCACTGGCGGCGGCCGACATCGCAGTGGGTGTGCTCGCCATC
CCCTTTGCCATCACCATCAGCACCGGGTTCTGCGCTGCCTGCCACGGCTGCCTCTTCATT
GCCTGCTTCGTCCTGGTCCTCACGCAGAGCTCCATCTTCAGTCTCCTGGCCATCGCCATT
GACCGCTACATTGCCATCCGCATCCCGCTCCGGTACAATGGCTTGGTGACCGGCACGAGG
GCTAAGGGCATCATTGCCATCTGCTGGGTGCTGTCGTTTGCCATCGGCCTGACTCCCATG
CTAGGTTGGAACAACTGCGGTCAGCCAAAGGAGGGCAAGAACCACTCCCAGGGCTGCGGG
GAGGGCCAAGTGGCCTGTCTCTTTGAGGATGTGGTCCCCATGAACTACATGGTGTACTTC
AACTTCTTTGCCTGTGTGCTGGTGCCCCTGCTGCTCATGCTGGGTGTCTATTTGCGGATC
TTCCTGGCGGCGCGACGACAGCTGAAGCAGATGGAGAGCCAGCCTCTGCCGGGGGAGCGG
GCACGGTCCACACTGCAGAAGGAGGTCCATGCTGCCAAGTCACTGGCCATCATTGTGGGG
CTCTTTGCCCTCTGCTGGCTGCCCCTACACATCATCAACTGCTTCACTTTCTTCTGCCCC
GACTGCAGCCACGCCCCTCTCTGGCTCATGTACCTGGCCATCGTCCTCTCCCACACCAAT
TCGGTTGTGAATCCCTTCATCTACGCCTACCGTATCCGCGAGTTCCGCCAGACCTTCCGC
AAGATCATTCGCAGCCACGTCCTGAGGCAGCAAGAACCTTTCAAGGCAGCTGGCACCAGT
GCCCGGGTCTTGGCAGCTCATGGCAGTGACGGAGAGCAGGTCAGCCTCCGTCTCAACGGC
CACCCGCCAGGAGTGTGGGCCAACGGCAGTGCTCCCCACCCTGAGCGGAGGCCCAATGGC
TATGCCCTGGGGCTGGTGAGTGGAGGGAGTGCCCAAGAGTCCCAGGGGAACACGGGCCTC
CCAGACGTGGAGCTCCTTAGCCATGAGCTCAAGGGAGTGTGCCCAGAGCCCCCTGGCCTA
GATGACCCCCTGGCCCAGGATGGAGCAGGAGTGTCCTGA
Chromosome Location
22
Locus
22q11.23
External Identifiers
ResourceLink
UniProtKB IDP29274
UniProtKB Entry NameAA2AR_HUMAN
GenBank Protein ID177892
GenBank Gene IDM97370
GenAtlas IDADORA2A
HGNC IDHGNC:263
General References
  1. Furlong TJ, Pierce KD, Selbie LA, Shine J: Molecular characterization of a human brain adenosine A2 receptor. Brain Res Mol Brain Res. 1992 Sep;15(1-2):62-6. [PubMed:1331670]
  2. Le F, Townsend-Nicholson A, Baker E, Sutherland GR, Schofield PR: Characterization and chromosomal localization of the human A2a adenosine receptor gene: ADORA2A. Biochem Biophys Res Commun. 1996 Jun 14;223(2):461-7. [PubMed:8670304]
  3. Collins JE, Wright CL, Edwards CA, Davis MP, Grinham JA, Cole CG, Goward ME, Aguado B, Mallya M, Mokrab Y, Huckle EJ, Beare DM, Dunham I: A genome annotation-driven approach to cloning the human ORFeome. Genome Biol. 2004;5(10):R84. Epub 2004 Sep 30. [PubMed:15461802]
  4. Ota T, Suzuki Y, Nishikawa T, Otsuki T, Sugiyama T, Irie R, Wakamatsu A, Hayashi K, Sato H, Nagai K, Kimura K, Makita H, Sekine M, Obayashi M, Nishi T, Shibahara T, Tanaka T, Ishii S, Yamamoto J, Saito K, Kawai Y, Isono Y, Nakamura Y, Nagahari K, Murakami K, Yasuda T, Iwayanagi T, Wagatsuma M, Shiratori A, Sudo H, Hosoiri T, Kaku Y, Kodaira H, Kondo H, Sugawara M, Takahashi M, Kanda K, Yokoi T, Furuya T, Kikkawa E, Omura Y, Abe K, Kamihara K, Katsuta N, Sato K, Tanikawa M, Yamazaki M, Ninomiya K, Ishibashi T, Yamashita H, Murakawa K, Fujimori K, Tanai H, Kimata M, Watanabe M, Hiraoka S, Chiba Y, Ishida S, Ono Y, Takiguchi S, Watanabe S, Yosida M, Hotuta T, Kusano J, Kanehori K, Takahashi-Fujii A, Hara H, Tanase TO, Nomura Y, Togiya S, Komai F, Hara R, Takeuchi K, Arita M, Imose N, Musashino K, Yuuki H, Oshima A, Sasaki N, Aotsuka S, Yoshikawa Y, Matsunawa H, Ichihara T, Shiohata N, Sano S, Moriya S, Momiyama H, Satoh N, Takami S, Terashima Y, Suzuki O, Nakagawa S, Senoh A, Mizoguchi H, Goto Y, Shimizu F, Wakebe H, Hishigaki H, Watanabe T, Sugiyama A, Takemoto M, Kawakami B, Yamazaki M, Watanabe K, Kumagai A, Itakura S, Fukuzumi Y, Fujimori Y, Komiyama M, Tashiro H, Tanigami A, Fujiwara T, Ono T, Yamada K, Fujii Y, Ozaki K, Hirao M, Ohmori Y, Kawabata A, Hikiji T, Kobatake N, Inagaki H, Ikema Y, Okamoto S, Okitani R, Kawakami T, Noguchi S, Itoh T, Shigeta K, Senba T, Matsumura K, Nakajima Y, Mizuno T, Morinaga M, Sasaki M, Togashi T, Oyama M, Hata H, Watanabe M, Komatsu T, Mizushima-Sugano J, Satoh T, Shirai Y, Takahashi Y, Nakagawa K, Okumura K, Nagase T, Nomura N, Kikuchi H, Masuho Y, Yamashita R, Nakai K, Yada T, Nakamura Y, Ohara O, Isogai T, Sugano S: Complete sequencing and characterization of 21,243 full-length human cDNAs. Nat Genet. 2004 Jan;36(1):40-5. Epub 2003 Dec 21. [PubMed:14702039]
  5. 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. [PubMed:15489334]
  6. Woods AS: The dopamine D(4) receptor, the ultimate disordered protein. J Recept Signal Transduct Res. 2010 Oct;30(5):331-6. doi: 10.3109/10799893.2010.513842. [PubMed:20836733]
  7. Kim J, Wess J, van Rhee AM, Schoneberg T, Jacobson KA: Site-directed mutagenesis identifies residues involved in ligand recognition in the human A2a adenosine receptor. J Biol Chem. 1995 Jun 9;270(23):13987-97. [PubMed:7775460]
  8. Milojevic T, Reiterer V, Stefan E, Korkhov VM, Dorostkar MM, Ducza E, Ogris E, Boehm S, Freissmuth M, Nanoff C: The ubiquitin-specific protease Usp4 regulates the cell surface level of the A2A receptor. Mol Pharmacol. 2006 Apr;69(4):1083-94. Epub 2005 Dec 9. [PubMed:16339847]
  9. Jaakola VP, Griffith MT, Hanson MA, Cherezov V, Chien EY, Lane JR, Ijzerman AP, Stevens RC: The 2.6 angstrom crystal structure of a human A2A adenosine receptor bound to an antagonist. Science. 2008 Nov 21;322(5905):1211-7. doi: 10.1126/science.1164772. Epub 2008 Oct 2. [PubMed:18832607]
  10. Cargill M, Altshuler D, Ireland J, Sklar P, Ardlie K, Patil N, Shaw N, Lane CR, Lim EP, Kalyanaraman N, Nemesh J, Ziaugra L, Friedland L, Rolfe A, Warrington J, Lipshutz R, Daley GQ, Lander ES: Characterization of single-nucleotide polymorphisms in coding regions of human genes. Nat Genet. 1999 Jul;22(3):231-8. [PubMed:10391209]

Drug Relations

Drug Relations
DrugBank IDNameDrug groupPharmacological action?ActionsDetails
DB00201CaffeineapprovedyesantagonistmultitargetDetails
DB04853BinodenosoninvestigationalunknownDetails
DB04932Defibrotideapproved, investigationalunknownDetails
DB05191Atl146einvestigationalunknownDetails
DB05009ApadenosoninvestigationalunknownDetails
DB00277TheophyllineapprovedyesantagonistDetails
DB06213Regadenosonapproved, investigationalyesagonistDetails
DB00358Mefloquineapproved, investigationalunknownantagonistDetails
DB00640Adenosineapproved, investigationalyesagonistDetails
DB087704-{2-[(7-amino-2-furan-2-yl[1,2,4]triazolo[1,5-a][1,3,5]triazin-5-yl)amino]ethyl}phenolexperimentalunknownDetails
DB00806Pentoxifyllineapproved, investigationalyesantagonistDetails
DB00651DyphyllineapprovedyesantagonistDetails
DB01303OxtriphyllineapprovedyesantagonistDetails
DB01412TheobromineinvestigationalyesantagonistDetails
DB00824Enprofyllineapproved, experimentalunknowninhibitorDetails
DB09273DoxofyllineexperimentalunknownantagonistDetails
DB00555Lamotrigineapproved, investigationalunknowninhibitorDetails
DB141328-chlorotheophyllineexperimentalyesantagonistDetails
DB11757Istradefyllineapproved, investigationalyesantagonistDetails