The adenosine A2B receptor, also known as ADORA2B, is a G-protein coupledadenosine 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]
^Volpini R, Costanzi S, Lambertucci C, Taffi S, Vittori S, Klotz KN, Cristalli G (July 2002). "N(6)-alkyl-2-alkynyl derivatives of adenosine as potent and selective agonists at the human adenosine A(3) receptor and a starting point for searching A(2B) ligands". Journal of Medicinal Chemistry. 45 (15): 3271–3279. doi:10.1021/jm0109762. PMID12109910.
^Baraldi PG, Tabrizi MA, Preti D, Bovero A, Romagnoli R, Fruttarolo F, et al. (March 2004). "Design, synthesis, and biological evaluation of new 8-heterocyclic xanthine derivatives as highly potent and selective human A2B adenosine receptor antagonists". Journal of Medicinal Chemistry. 47 (6): 1434–1447. doi:10.1021/jm0309654. PMID14998332.
^Beukers MW, Meurs I, Ijzerman AP (September 2006). "Structure-affinity relationships of adenosine A2B receptor ligands". Medicinal Research Reviews. 26 (5): 667–698. doi:10.1002/med.20069. PMID16847822. S2CID24390495.
^Elzein E, Kalla R, Li X, Perry T, Parkhill E, Palle V, et al. (January 2006). "Novel 1,3-dipropyl-8-(1-heteroarylmethyl-1H-pyrazol-4-yl)-xanthine derivatives as high affinity and selective A2B adenosine receptor antagonists". Bioorganic & Medicinal Chemistry Letters. 16 (2): 302–306. doi:10.1016/j.bmcl.2005.10.002. PMID16275090.
^Carotti A, Cadavid MI, Centeno NB, Esteve C, Loza MI, Martinez A, et al. (January 2006). "Design, synthesis, and structure-activity relationships of 1-,3-,8-, and 9-substituted-9-deazaxanthines at the human A2B adenosine receptor". Journal of Medicinal Chemistry. 49 (1): 282–299. doi:10.1021/jm0506221. PMID16392813.
^Tabrizi MA, Baraldi PG, Preti D, Romagnoli R, Saponaro G, Baraldi S, et al. (March 2008). "1,3-Dipropyl-8-(1-phenylacetamide-1H-pyrazol-3-yl)-xanthine derivatives as highly potent and selective human A(2B) adenosine receptor antagonists". Bioorganic & Medicinal Chemistry. 16 (5): 2419–2430. doi:10.1016/j.bmc.2007.11.058. PMID18077171.
^Stefanachi A, Brea JM, Cadavid MI, Centeno NB, Esteve C, Loza MI, et al. (March 2008). "1-, 3- and 8-substituted-9-deazaxanthines as potent and selective antagonists at the human A2B adenosine receptor". Bioorganic & Medicinal Chemistry. 16 (6): 2852–2869. doi:10.1016/j.bmc.2008.01.002. PMID18226909.
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. doi:10.1016/S0006-291X(05)81462-7. PMID1325798.
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. doi:10.1006/geno.1995.1061. PMID7558011.
Townsend-Nicholson A, Baker E, Sutherland GR, Schofield PR (January 1995). "Localization of the adenosine A2b receptor subtype gene (ADORA2B) to chromosome 17p11.2-p12 by FISH and PCR screening of somatic cell hybrids". Genomics. 25 (2): 605–607. doi:10.1016/0888-7543(95)80074-V. PMID7790006.
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. PMID8022409.
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. doi:10.1242/jcs.112.4.491. PMID9914161.
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. PMID10101031.
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. Bibcode:2000Natur.407..747C. doi:10.1038/35037600. PMID11048721. S2CID4423128.
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. doi:10.1124/mol.59.1.127. PMID11125033.
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. doi:10.1002/cne.1334. PMID11579381. S2CID46222306.
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. doi:10.1021/jm011049y. PMID11906291.
"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.
