腺苷A_2A受體

腺苷A2A受体
已知的结构
PDB	直系同源搜索: PDBe RCSB
PDBID列表
	2YDO、2YDV、3EML、3PWH、3QAK、3REY、3RFM、3UZA、3UZC、3VG9、3VGA、4EIY、4UG2、4UHR、5IU4、5IU7、5IUA、5IU8、5IUB
识别号
别名	ADORA2A；, adenosine A2a receptor, A2aR, ADORA2, RDC8
外部ID	OMIM：102776 MGI：99402 HomoloGene：20166 GeneCards：ADORA2A
为以下药物的标靶
	腺苷、BAY 60-6583、Regadenoson、UK-432,097、CCPA、CGS-21680、cyclopentyladenosine、咖啡因、CGS 15943、8-环戊基-1,3-二丙基黄嘌呤、flavone、高良姜素、istradefylline、桑色素、瑞德南特、rolofylline、樱花素、sch-442416、sch-58261、茶碱、ZM-241385
基因位置（人类）
染色体	22号染色体
终止	24,442,357 bp
基因位置（小鼠）
染色体	小鼠10号染色体
终止	75,170,618 bp
RNA表达模式
	查阅更多表达数据
基因本体
分子功能	• G protein-coupled adenosine receptor activity; • G protein-coupled receptor activity; • signal transducer activity; • 血浆蛋白结合; • 相同蛋白质结合; • 酶结合; • alpha-actinin binding; • type 5 metabotropic glutamate receptor binding; • protein heterodimerization activity;
细胞组分	• integral component of membrane; • 膜; • 细胞膜; • integral component of plasma membrane; • 中间纤维; • 内膜系统; • 突触后致密物质; • 轴突; • 树突; • axolemma; • asymmetric synapse; • presynaptic membrane; • soma; • postsynaptic membrane; • presynaptic active zone; • integral component of postsynaptic membrane; • integral component of presynaptic membrane; • glutamatergic synapse; • Golgi membrane;
生物学过程	• cAMP biosynthetic process; • G protein-coupled adenosine receptor signaling pathway; • sensory perception; • adenylate cyclase-modulating G protein-coupled receptor signaling pathway; • cell-cell signaling; • 凝血; • blood circulation; • cellular defense response; • central nervous system development; • 吞噬作用; • inflammatory response; • 信号转导; • 细胞凋亡; • synaptic transmission, dopaminergic; • response to amphetamine; • regulation of transcription, DNA-templated; • negative regulation of protein kinase activity; • protein kinase C-activating G protein-coupled receptor signaling pathway; • synaptic transmission, cholinergic; • locomotory behavior; • negative regulation of cell population proliferation; • positive regulation of glutamate secretion; • positive regulation of acetylcholine secretion, neurotransmission; • regulation of norepinephrine secretion; • response to caffeine; • positive regulation of synaptic transmission, GABAergic; • synaptic transmission, glutamatergic; • positive regulation of urine volume; • positive regulation of renal sodium excretion; • negative regulation of locomotion; • 血管舒张; • eating behavior; • negative regulation of vascular permeability; • negative regulation of cysteine-type endopeptidase activity involved in apoptotic process; • response to alkaloid; • negative regulation of neuron apoptotic process; • positive regulation of circadian sleep/wake cycle, sleep; • negative regulation of alpha-beta T cell activation; • astrocyte activation; • neuron projection morphogenesis; • positive regulation of protein secretion; • negative regulation of inflammatory response; • regulation of mitochondrial membrane potential; • membrane depolarization; • regulation of calcium ion transport; • positive regulation of synaptic transmission, glutamatergic; • 兴奋性动作电位; • 抑制性突触; • 前脉冲抑制; • positive regulation of apoptotic signaling pathway; • G protein-coupled receptor signaling pathway; • adenylate cyclase-activating G protein-coupled receptor signaling pathway; • positive regulation of long-term synaptic potentiation; • regulation of synaptic vesicle exocytosis;
	Sources:Amigo / QuickGO
直系同源
	135
	11540
	ENSG00000128271
	ENSMUSG00000020178
	P29274
	Q60613
	NM_000675; NM_001278497; NM_001278498; NM_001278499; NM_001278500
	NM_009630; NM_001331095; NM_001331096
	NP_000666; NP_001265426; NP_001265427; NP_001265428; NP_001265429
	NP_001318024; NP_001318025; NP_033760
	维基数据
查看/编辑人类	查看/编辑小鼠

腺苷A_2A受体(adenosine A_2A receptor)，也称为ADORA2A，是一种腺苷受体，也表示编码它的人类基因。^[6]^[7]

参考资料

^ 對Adenosine A2a receptor起作用的藥物；在維基數據上查看/編輯參考.
^ ^2.0 ^2.1 ^2.2 GRCh38: Ensembl release 89: ENSG00000128271 - Ensembl, May 2017
^ ^3.0 ^3.1 ^3.2 GRCm38: Ensembl release 89: ENSMUSG00000020178 - Ensembl, May 2017
^ Human PubMed Reference:. National Center for Biotechnology Information, U.S. National Library of Medicine.
^ Mouse PubMed Reference:. National Center for Biotechnology Information, U.S. National Library of Medicine.
^ Libert F, Parmentier M, Lefort A, Dinsart C, Van Sande J, Maenhaut C, et al. Selective amplification and cloning of four new members of the G protein-coupled receptor family. Science. May 1989, 244 (4904): 569–72. Bibcode:1989Sci...244..569L. PMID 2541503. doi:10.1126/science.2541503.
^ Libert F, Passage E, Parmentier M, Simons MJ, Vassart G, Mattei MG. Chromosomal mapping of A1 and A2 adenosine receptors, VIP receptor, and a new subtype of serotonin receptor. Genomics. September 1991, 11 (1): 225–7. PMID 1662665. doi:10.1016/0888-7543(91)90125-X.

深入阅读

Russo EB. Taming THC: potential cannabis synergy and phytocannabinoid-terpenoid entourage effects. British Journal of Pharmacology. August 2011, 163 (7): 1344–64. PMC 3165946 . PMID 21749363. doi:10.1111/j.1476-5381.2011.01238.x.
Ongini E, Adami M, Ferri C, Bertorelli R. Adenosine A2A receptors and neuroprotection. Annals of the New York Academy of Sciences. October 1997, 825 (1 Neuroprotecti): 30–48. Bibcode:1997NYASA.825...30O. PMID 9369973. doi:10.1111/j.1749-6632.1997.tb48412.x.
Furlong TJ, Pierce KD, Selbie LA, Shine J. Molecular characterization of a human brain adenosine A2 receptor. Brain Research. Molecular Brain Research. September 1992, 15 (1–2): 62–6. PMID 1331670. doi:10.1016/0169-328X(92)90152-2.
Makujina SR, Sabouni MH, Bhatia S, Douglas FL, Mustafa SJ. Vasodilatory effects of adenosine A2 receptor agonists CGS 21680 and CGS 22492 in human vasculature. European Journal of Pharmacology. October 1992, 221 (2–3): 243–7. PMID 1426003. doi:10.1016/0014-2999(92)90708-C.
Karlsten R, Gordh T, Post C. Local antinociceptive and hyperalgesic effects in the formalin test after peripheral administration of adenosine analogues in mice. Pharmacology & Toxicology. June 1992, 70 (6 Pt 1): 434–8. PMID 1438021. doi:10.1111/j.1600-0773.1992.tb00503.x.
Libert F, Passage E, Parmentier M, Simons MJ, Vassart G, Mattei MG. Chromosomal mapping of A1 and A2 adenosine receptors, VIP receptor, and a new subtype of serotonin receptor. Genomics. September 1991, 11 (1): 225–7. PMID 1662665. doi:10.1016/0888-7543(91)90125-X.
Martinez-Mir MI, Probst A, Palacios JM. Adenosine A2 receptors: selective localization in the human basal ganglia and alterations with disease. Neuroscience. 1992, 42 (3): 697–706. PMID 1835521. S2CID 23693441. doi:10.1016/0306-4522(91)90038-P.
Libert F, Parmentier M, Lefort A, Dinsart C, Van Sande J, Maenhaut C, et al. Selective amplification and cloning of four new members of the G protein-coupled receptor family. Science. May 1989, 244 (4904): 569–72. Bibcode:1989Sci...244..569L. PMID 2541503. doi:10.1126/science.2541503.
Kim J, Wess J, van Rhee AM, Schöneberg T, Jacobson KA. Site-directed mutagenesis identifies residues involved in ligand recognition in the human A2a adenosine receptor. The Journal of Biological Chemistry. June 1995, 270 (23): 13987–97. PMC 3427751 . PMID 7775460. doi:10.1074/jbc.270.23.13987.
Szondy Z. Adenosine stimulates DNA fragmentation in human thymocytes by Ca(2+)-mediated mechanisms. The Biochemical Journal. 304. December 1994,. 304 ( Pt 3) (3): 877–85. PMC 1137415 . PMID 7818494. doi:10.1042/bj3040877.
MacCollin M, Peterfreund R, MacDonald M, Fink JS, Gusella J. Mapping of a human A2a adenosine receptor (ADORA2) to chromosome 22. Genomics. March 1994, 20 (2): 332–3. PMID 8020991. doi:10.1006/geno.1994.1181.
Nonaka H, Ichimura M, Takeda M, Nonaka Y, Shimada J, Suzuki F, et al. KF17837 ((E)-8-(3,4-dimethoxystyryl)-1,3-dipropyl-7-methylxanthine), a potent and selective adenosine A2 receptor antagonist. European Journal of Pharmacology. May 1994, 267 (3): 335–41. PMID 8088373. doi:10.1016/0922-4106(94)90159-7.
Iwamoto T, Umemura S, Toya Y, Uchibori T, Kogi K, Takagi N, Ishii M. Identification of adenosine A2 receptor-cAMP system in human aortic endothelial cells. Biochemical and Biophysical Research Communications. March 1994, 199 (2): 905–10. PMID 8135838. doi:10.1006/bbrc.1994.1314.
Salmon JE, Brogle N, Brownlie C, Edberg JC, Kimberly RP, Chen BX, Erlanger BF. Human mononuclear phagocytes express adenosine A1 receptors. A novel mechanism for differential regulation of Fc gamma receptor function. Journal of Immunology. September 1993, 151 (5): 2775–85. PMID 8360491.
Peterfreund RA, MacCollin M, Gusella J, Fink JS. Characterization and expression of the human A2a adenosine receptor gene. Journal of Neurochemistry. January 1996, 66 (1): 362–8. PMID 8522976. doi:10.1046/j.1471-4159.1996.66010362.x.
Le F, Townsend-Nicholson A, Baker E, Sutherland GR, Schofield PR. Characterization and chromosomal localization of the human A2a adenosine receptor gene: ADORA2A. Biochemical and Biophysical Research Communications. June 1996, 223 (2): 461–7. PMID 8670304. doi:10.1006/bbrc.1996.0916.
Jiang Q, Van Rhee AM, Kim J, Yehle S, Wess J, Jacobson KA. Hydrophilic side chains in the third and seventh transmembrane helical domains of human A2A adenosine receptors are required for ligand recognition. Molecular Pharmacology. September 1996, 50 (3): 512–21. PMC 3418326 . PMID 8794889.
Ledent C, Vaugeois JM, Schiffmann SN, Pedrazzini T, El Yacoubi M, Vanderhaeghen JJ, et al. Aggressiveness, hypoalgesia and high blood pressure in mice lacking the adenosine A2a receptor. Nature. August 1997, 388 (6643): 674–8. Bibcode:1997Natur.388..674L. PMID 9262401. S2CID 2662174. doi:10.1038/41771.
Koshiba M, Rosin DL, Hayashi N, Linden J, Sitkovsky MV. Patterns of A2A extracellular adenosine receptor expression in different functional subsets of human peripheral T cells. Flow cytometry studies with anti-A2A receptor monoclonal antibodies. Molecular Pharmacology. March 1999, 55 (3): 614–24. PMID 10051547.
Borgland SL, Castañón M, Spevak W, Parkinson FE. Effects of propentofylline on adenosine receptor activity in Chinese hamster ovary cell lines transfected with human A1, A2A, or A2B receptors and a luciferase reporter gene. Canadian Journal of Physiology and Pharmacology. December 1998, 76 (12): 1132–8. PMID 10326835. doi:10.1139/cjpp-76-12-1132.

外部链接

Human ADORA2A genome location and ADORA2A gene details page in the UCSC Genome Browser（英语：UCSC Genome Browser）.

[1] 對Adenosine A2a receptor起作用的藥物；在維基數據上查看/編輯參考.

[refGRCh38Ensembl-2] 2.0 ^2.1 ^2.2 GRCh38: Ensembl release 89: ENSG00000128271 - Ensembl, May 2017

[refGRCm38Ensembl-3] 3.0 ^3.1 ^3.2 GRCm38: Ensembl release 89: ENSMUSG00000020178 - Ensembl, May 2017

[4] Human PubMed Reference:. National Center for Biotechnology Information, U.S. National Library of Medicine.

[5] Mouse PubMed Reference:. National Center for Biotechnology Information, U.S. National Library of Medicine.

[pmid2541503-6] Libert F, Parmentier M, Lefort A, Dinsart C, Van Sande J, Maenhaut C, et al. Selective amplification and cloning of four new members of the G protein-coupled receptor family. Science. May 1989, 244 (4904): 569–72. Bibcode:1989Sci...244..569L. PMID 2541503. doi:10.1126/science.2541503.

[pmid1662665-7] Libert F, Passage E, Parmentier M, Simons MJ, Vassart G, Mattei MG. Chromosomal mapping of A1 and A2 adenosine receptors, VIP receptor, and a new subtype of serotonin receptor. Genomics. September 1991, 11 (1): 225–7. PMID 1662665. doi:10.1016/0888-7543(91)90125-X.

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