Abstract
Prior to the application of recombinant DNA technology, the characterization of adenosine receptor subtypes was limited to information obtained from classic pharmacological analysis. Through the use of gene cloning and molecular biologic techniques, we have significantly advanced our understanding of the number of adenosine receptor subtypes and their molecular characteristics, such as primary sequence, structural homology between species, pharmacologic profiles of agonists and antagonists, and distribution of tissue and cellular expression. Molecular cloning has confirmed the existence of three adenosine receptor subtypes predicted from affinity order profiles of agonists and antagonists, and coupling to adenylyl cyclase, and, in addition, has identified a fourth subtype that had previously remained pharmacologically undetected. In this overview progress in the cloning and molecular characterization of adenosine receptors will be summarized.
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References
Van Calker D, Muller M, Hamprecht B (1979) Adenosine regulates via two different types of receptors, the accumulation of cyclic AMP in cultured brain cells. J Neurochem 33:999–1005.
Daly JW, Butts-Lamb P, Padgett W (1983) Subclasses of adenosine receptors in the central nervous system: Interaction with caffeine and related methylxanthines. Cell Mol Neurobiol 3:69–80.
Bruns RF, Lu GH, Pugsley TA (1986) Characterization of the A2 adenosine receptor labeled by [3H]NECA in rat striatal membranes. Mol Pharmacol 29:331–346.
Jacobson KA, van Galen PJM, Williams M (1992) Adenosine receptors: Pharmacology, structure-activity relationship and therapeutic potential. J Med Chem 35:407–422.
Libert F, Parmentier M, Lefort A, Dinsart C, Van Sande J, Maenhaut C, Simons M, Dumont JE, Vassart G (1989) Selective amplification and cloning of four new members of the G protein-coupled receptor family. Science 244:569–572
Libert F, Schiffmann SN, Lefort A, Parmentier M, Vanderhaeghen J J, Vassart G (1991) The orphan receptor cDNA RDC7 encodes an A1 adenosine receptor. EMBO J 10:1677–1682.
Maenhaut C, Van Sande J, Libert F, Abramowicz M, Parmentier M, Vanderhaeghen JJ, Dumont JE, Vassart G, Schiffmann S (1990) RDC8 codes for an adenosine A2 receptor with physiological constitutive activity. Biochem Biophys Res Comm 173:1169–1178.
Stehle JH, Rivkees SA, Lee JJ, Weaver DR, Deeds JD, Reppert SM (1992) Molecular cloning and expression of the cDNA for a novel A2-adenosine receptor subtype. Mol Endocrinol 6:384–393.
Rivkees SA, Reppert SM (1992) RFL9 encodes an A2b-adenosine receptor. Mol Endocrinol 6: 1598–1604.
Meyerhof W, Muller-Brechlin R, Richter D (1991) Molecular cloning of a novel putative G-protein coupled receptor expressed during rat spermiogenesis. FEBS Lett 284:155–160.
Zhou Q-Y, Chuanyi L, Olah ME, Johnson RA, Stiles GL, Civelli O (1992) Molecular cloning and characterization of an adenosine receptor: The A3 adenosine receptor. Proc Natl Acad Sci USA 89:7432–7436.
Ribeiro JA, Sebastiao AM (1986) Adenosine receptors and calcium: Basis for proposing a third (A3) adenosine receptor. Prog Neurobiol 26:179–209.
Bruns RF, Daly JW, Snyder SH (1980) Adenosine receptors in brain membranes: Binding of N6-cyclohexyl[3H]adenosine and 1,3diethy1–8-{3H]phenylxanthine. Proc Natl Acad Sci USA 77:5547–5551.
Wan W, Sutherland GR, Geiger JD (1990) Binding of the adenosine A2 receptor ligand [3H]CGS21680 to human and rat brain: Evidence for multiple affinity sites. J Neurochem 55:1763–1771.
Salvatore CA, Luneau CJ, Johnson RG, Jacobson MA (1992) Molecular cloning and characterization of human A1 and A2 adenosine receptors. Int J Pur Pyrid Res 3:82.
Ukena D, Jacobson KA, Padgett WL, Ayala C, Shamim MT, Kirk KL, Olsson RO, Daly JW (1986) Species differences in the structure-activity relationships of adenosine agonists and xanthine antagonists at brain A1 adenosine receptors. FEBS Lett 209:122–128.
Stone GA, Jarvis MF, Sills MA, Weeks B, Snowhill EW, Williams M (1988) Species differences in high-affinity adenosine A2 binding sites in striatal membranes from mammalian brain. Drug Dev Res 15:31–46.
Probst WC, Snyder LA, Schuster DI, Brosius J, Sealfon SC (1992) Sequence alignment of the G-protein coupled receptor superfamily. DNA Cell Biol 11:1–20.
O’Dowd BF, Hnatowich M, Caron MG, Lefkowitz RJ, Bouvier M (1989) Palmitoylation of the human ß2-adrenergic receptor. J Biol Chem 264:7564–7569.
Olah ME, Ren H, Ostrowski J, Jacobson KA, Stiles GL (1992) Cloning, expression and characterization of the unique bovine A1 adenosine receptor. J Biol Chem 267:10764–10770.
Klotz K-N, Lohse MJ, Schwabe U (1988) Chemical modification of A1 adenosine receptors in rat brain membranes. J Biol Chem 263: 17522–17526
Townsend-Nicholson A, Schofield PR (1994) A threonine residue in the seventh transmembrane domain of the human A1 adenosine receptor mediates specific agonist binding. J Biol Chem 269:2373–2376.
Salvatore CA, Jacobson MA, Taylor HE, Linden J, Johnson RG (1993) Molecular cloning and characterization of the human A3 adenosine receptor. Proc Natl Acad Sci USA 90:10365–10369.
Linden J, Taylor HE, Robeva AS, Tucker AL, Stehle JH, Rivkees SA, Fink SJ, Reppert SM (1993) Molecular cloning and functional expression of a sheep A3 adenosine receptor with widespread tissue distribution. Mol Pharm 44: 524–532.
Bhattacharya S, Dewitt DL, Burnatowska-Hledinn M, Smith WL, Spielman WS (1993) Cloning of an adenosine A1 receptor-encoding gene from rabbit. Gene 128:285–288.
Ren H, Stiles GL (1994) Characterization of the human A1 adenosine receptor gene. J Biol Chem 269:3104–3110.
Peterfreund RA, MacCollin M, Gusella J, Fink JS (1994) Structure of the human A2a receptor gene. Drug Dev Res 31:306.
Libert F, Passage E, Parmentier M, Simons M, Vassart G, Mattei M (1991) Chromosomal mapping of A1 and A2 adenosine receptors, VIP receptor and a new subtype of serotonin receptor. Genomics 11:225–227.
MacCollin M, Peterfreund R, MacDonald M, Fink JS, Guesella J (1994) Mapping of a human A2a adenosine receptor (ADORA2) to chromosome 22. Genomics 20:332–333.
Rivkees SA, Reppert SM, Wells HB (1994) Molecular cloning and characterization of a human A1-adenosine receptor. Drug Dev Res 31:314.
Schiffman SN, Libert F, Vassart G, Vanderhaeghen J J (1991) Distribution of adenosine A2 receptor mRNA in the human brain. Neurosci Lett 130:177–181.
Schiffman SN, Libert F, Vassart G, Dumont JE, Vanderhaeghen JJ (1990) A cloned G protein-coupled protein with a distribution restricted to striatal medium-sized neurons. Possible relationship with D1 dopamine receptor. Brain Res 519:333–337.
Fastbom J, Pazos A, Probst A, Palacious JM (1986) Adenosine A1-receptors in human brain: Characterization and autoradiographic visualization. Neurosci Lett 65:127–132.
Martinez-Mir MI, Probst A, Palacious JM (1991) Adenosine A2 receptors: Selective localization in the human basal ganglia and alterations with disease. Neuroscience 42:697–706.
Libert F, Van Sande J, Lefort A, Czernilofsky A, Dumont JE, Vassart G, Ensinger HA, Mendia KD (1992) Cloning and functional characterization of a human A1 adenosine receptor. Biochem Biophys Res Comm 187:919–926.
Mahan LC, McVittie LD, Smyk-Randall EM, Nakata H, Monsma FJ, Gerfen CR, Sibley DR (1991) Cloning and expression of an A1 adenosine receptor from rat brain. Mol Pharmacol 40:1–7.
Reppert SM, Weaver DR, Stehle JH, Rivkees SA (1991) Molecular cloning and characterization of a rat A1 adenosine receptor that is widely expressed in brain and spinal cord. Mol Endocrinol 5:1037–1048.
Tucker AL, Linden J, Robeva AS, D’Angelo DD, Lynch KR (1992) Cloning and expression of a bovine adenosine A1 receptor cDNA. FEBS Lett 297:107–111.
Marquardt DL, Walker LL, Heinemann S (1994) Cloning of two adenosine receptor subtypes from mouse bone marrow-derived mast cells. J Immunol 152:4508–4515.
Furlong TJ, Pierce KD, Selbie LA, Shine J (1992) Molecular characterization of a human brain adenosine A2 receptor. Mol Brain Res 15:62–66.
Meng F, Xie G, Chalmers D, Morgan C, Watson SJ, Akil H (1994) Cloning and expression of the A2a adenosine receptor from guinea pig brain. Neurochem Res 19:613–621.
Fink JS, Weaver DR, Rivkees SA, Peterfreund RA, Pollack AE, Adler EM, Reppert SM (1992) Molecular cloning of the rat A2 receptor: Selective co-expression with D2 dopamine receptors in rat striatum. Mol Brain Res 14:186–195.
Chern Y, King K, Lai H (1992) Molecular cloning of a novel adenosine receptor gene from rat brain. Biochem Biophys Res Comm 185: 304–309.
Pierce KD, Furlong TJ, Selbie LA, Shine J (1992) Molecular cloning and expression of an adenosine A2b receptor from human brain. Biochem Biophys Res Comm 187:86–93.
Sajjadi F, Firestein GS (1993) cDNA cloning and sequence analysis of the human A3 adenosine receptor. Biochem Biophys Acta 1179:105–107.
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Jacobson, M.A. (1995). Molecular Biology of Adenosine Receptors. In: Belardinelli, L., Pelleg, A. (eds) Adenosine and Adenine Nucleotides: From Molecular Biology to Integrative Physiology. Springer, Boston, MA. https://doi.org/10.1007/978-1-4615-2011-5_1
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DOI: https://doi.org/10.1007/978-1-4615-2011-5_1
Publisher Name: Springer, Boston, MA
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