Adenosine A2B receptor
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Adenosine A2b receptor
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| Location (UCSC) | Chr 17: 15.95 – 15.98 Mb | Chr 11: 62.14 – 62.16 Mb | |||||||
| PubMed search | [3] | [4] | |||||||
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The adenosine A2B receptor, also known as ADORA2B, is a G-protein coupled adenosine receptor, and also denotes the human adenosine A2b receptor gene which encodes it.[5]
Mechanism
This integral membrane protein stimulates adenylate cyclase activity in the presence of adenosine. This protein also interacts with netrin-1, which is involved in axon elongation.
Gene
The gene is located near the Smith-Magenis syndrome region on chromosome 17.[5]
Ligands
Research into selective A2B ligands has lagged somewhat behind the development of ligands for the other three adenosine receptor subtypes, but a number of A2B-selective compounds have now been developed,[6][7][8][9][10][11][12][13][14][15] and research into their potential therapeutic applications is ongoing.[16][17][18][19][20][21][22]
Agonists
- BAY 60-6583
- NECA (N-ethylcarboxamidoadenosine)
- (S)-PHPNECA - high affinity and efficacy at A2B, but poor selectivity over other adenosine receptor subtypes
- LUF-5835
- LUF-5845 - partial agonist
Antagonists and inverse agonists
- Compound 38:[23] antagonist, high affinity and good subtype selectivity
- ISAM-R56A:[22] non-xanthinic high affinity selective antagonist (Ki: 1.50 nM)
- ISAM-140:[24] non-xanthinic selective antagonist (Ki = 3.49 nM).
- ISAM-R324A:[25] Soluble and metabolically stable non-xanthinic selective antagonist (Ki = 6.10 nM).
- ATL-801
- CVT-6883
- MRS-1706
- MRS-1754
- OSIP-339,391
- PSB-603: xanthinic antagonist
- PSB-0788: xanthinic antagonist
- PSB-1115: xanthinic antagonist
- PSB-1901:[26] xanthinic antagonist with picomolar potency
References
- ^ a b c GRCh38: Ensembl release 89: ENSG00000170425 – Ensembl, May 2017
- ^ a b c GRCm38: Ensembl release 89: ENSMUSG00000018500 – 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.
- ^ a b "Entrez Gene: ADORA2B adenosine A2b receptor".
- PMID 12109910.
- PMID 12369946. Archived from the originalon 2013-04-14.
- PMID 14998332.
- PMID 16375751. Archived from the originalon 2013-04-14.
- PMID 17168717. Archived from the originalon 2013-04-14.
- S2CID 24390495.
- PMID 16275090.
- PMID 16392813.
- PMID 18077171.
- PMID 18226909.
- PMID 12570760. Archived from the originalon 2013-04-14.
- S2CID 13777846.
- PMID 18536750.
- PMID 18758473.
- PMID 19075778. Archived from the originalon 2013-04-14.
- S2CID 11066973.
- ^ PMID 35580926.
- PMID 18938084.
- PMID 26824742.
- PMID 36517209.
- S2CID 73472174.
Further reading
- Stiles GL (April 1992). "Adenosine receptors". The Journal of Biological Chemistry. 267 (10): 6451–6454. PMID 1551861.
- Pierce KD, Furlong TJ, Selbie LA, Shine J (August 1992). "Molecular cloning and expression of an adenosine A2b receptor from human brain". Biochemical and Biophysical Research Communications. 187 (1): 86–93. PMID 1325798.
- Li Q, Han X, Lan X, Hong X, Li Q, Gao Y, et al. (December 2017). "Inhibition of tPA-induced hemorrhagic transformation involves adenosine A2b receptor activation after cerebral ischemia". Neurobiology of Disease. 108: 173–182. PMID 28830843.
- Jacobson MA, Johnson RG, Luneau CJ, Salvatore CA (May 1995). "Cloning and chromosomal localization of the human A2b adenosine receptor gene (ADORA2B) and its pseudogene". Genomics. 27 (2): 374–376. PMID 7558011.
- Townsend-Nicholson A, Baker E, PMID 7790006.
- Strohmeier GR, Reppert SM, Lencer WI, Madara JL (February 1995). "The A2b adenosine receptor mediates cAMP responses to adenosine receptor agonists in human intestinal epithelia". The Journal of Biological Chemistry. 270 (5): 2387–2394. PMID 7836474.
- Feoktistov I, Murray JJ, Biaggioni I (June 1994). "Positive modulation of intracellular Ca2+ levels by adenosine A2b receptors, prostacyclin, and prostaglandin E1 via a cholera toxin-sensitive mechanism in human erythroleukemia cells". Molecular Pharmacology. 45 (6): 1160–1167. PMID 8022409.
- Mirabet M, Herrera C, Cordero OJ, Mallol J, Lluis C, Franco R (February 1999). "Expression of A2B adenosine receptors in human lymphocytes: their role in T cell activation". Journal of Cell Science. 112 ( Pt 4) (4): 491–502. PMID 9914161.
- Feoktistov I, Goldstein AE, Biaggioni I (April 1999). "Role of p38 mitogen-activated protein kinase and extracellular signal-regulated protein kinase kinase in adenosine A2B receptor-mediated interleukin-8 production in human mast cells". Molecular Pharmacology. 55 (4): 726–734. PMID 10101031.
- Corset V, Nguyen-Ba-Charvet KT, Forcet C, Moyse E, Chédotal A, Mehlen P (October 2000). "Netrin-1-mediated axon outgrowth and cAMP production requires interaction with adenosine A2b receptor". Nature. 407 (6805): 747–750. S2CID 4423128.
- Herrera C, Casadó V, Ciruela F, Schofield P, Mallol J, Lluis C, Franco R (January 2001). "Adenosine A2B receptors behave as an alternative anchoring protein for cell surface adenosine deaminase in lymphocytes and cultured cells". Molecular Pharmacology. 59 (1): 127–134. PMID 11125033.
- Christofi FL, Zhang H, Yu JG, Guzman J, Xue J, Kim M, et al. (October 2001). "Differential gene expression of adenosine A1, A2a, A2b, and A3 receptors in the human enteric nervous system". The Journal of Comparative Neurology. 439 (1): 46–64. S2CID 46222306.
- Hayallah AM, Sandoval-Ramírez J, Reith U, Schobert U, Preiss B, Schumacher B, et al. (March 2002). "1,8-disubstituted xanthine derivatives: synthesis of potent A2B-selective adenosine receptor antagonists". Journal of Medicinal Chemistry. 45 (7): 1500–1510. PMID 11906291.
- Sitaraman SV, Wang L, Wong M, Bruewer M, Hobert M, Yun CH, et al. (September 2002). "The adenosine 2b receptor is recruited to the plasma membrane and associates with E3KARP and Ezrin upon agonist stimulation". The Journal of Biological Chemistry. 277 (36): 33188–33195. PMID 12080047.
- Feoktistov I, Ryzhov S, Goldstein AE, Biaggioni I (March 2003). "Mast cell-mediated stimulation of angiogenesis: cooperative interaction between A2B and A3 adenosine receptors". Circulation Research. 92 (5): 485–492. S2CID 10346424.
- Eltzschig HK, Ibla JC, Furuta GT, Leonard MO, Jacobson KA, Enjyoji K, et al. (September 2003). "Coordinated adenine nucleotide phosphohydrolysis and nucleoside signaling in posthypoxic endothelium: role of ectonucleotidases and adenosine A2B receptors". The Journal of Experimental Medicine. 198 (5): 783–796. PMID 12939345.
- Ryzhov S, Goldstein AE, Matafonov A, Zeng D, Biaggioni I, Feoktistov I (June 2004). "Adenosine-activated mast cells induce IgE synthesis by B lymphocytes: an A2B-mediated process involving Th2 cytokines IL-4 and IL-13 with implications for asthma". Journal of Immunology. 172 (12): 7726–7733. PMID 15187156.
- Kolachala V, Asamoah V, Wang L, Srinivasan S, Merlin D, Sitaraman SV (February 2005). "Interferon-gamma down-regulates adenosine 2b receptor-mediated signaling and short circuit current in the intestinal epithelia by inhibiting the expression of adenylate cyclase". The Journal of Biological Chemistry. 280 (6): 4048–4057. PMID 15550390.
External links
- "Adenosine Receptors: A2B". IUPHAR Database of Receptors and Ion Channels. International Union of Basic and Clinical Pharmacology. Archived from the original on 2016-03-03. Retrieved 2008-11-25.
- Human ADORA2B genome location and ADORA2B gene details page in the UCSC Genome Browser.