메뉴 건너뛰기




Volumn 84, Issue 1, 2012, Pages 76-87

The role of the second and third extracellular loops of the adenosine A1 receptor in activation and allosteric modulation

Author keywords

Adenosine A1 receptor; Extracellular loops; G protein coupled receptor; Receptor activation; S. cerevisiae

Indexed keywords

2 AMINO 4,5 DIMETHYL 3 (3 TRIFLUOROMETHYLBENZOYL)THIOPHENE; ADENOSINE A1 RECEPTOR; ALANINE; G PROTEIN COUPLED RECEPTOR; GLUTAMIC ACID; TRYPTOPHAN;

EID: 84860671694     PISSN: 00062952     EISSN: 18732968     Source Type: Journal    
DOI: 10.1016/j.bcp.2012.03.008     Document Type: Article
Times cited : (53)

References (44)
  • 1
    • 0038024615 scopus 로고    scopus 로고
    • The G-protein-coupled receptors in the human genome form five main families, phylogenetic analysis, paralogon groups, and fingerprints
    • R. Fredriksson, M.C. Lagerstrom, L.G. Lundin, and H.B. Schioth The G-protein-coupled receptors in the human genome form five main families, phylogenetic analysis, paralogon groups, and fingerprints Mol Pharmacol 63 2003 1256 1272
    • (2003) Mol Pharmacol , vol.63 , pp. 1256-1272
    • Fredriksson, R.1    Lagerstrom, M.C.2    Lundin, L.G.3    Schioth, H.B.4
  • 2
    • 79551650974 scopus 로고    scopus 로고
    • GPCR structure and activation: An essential role for the first extracellular loop in activating the adenosine A2B receptor
    • M.C. Peeters, G.J. van Westen, D. Guo, L.E. Wisse, C.E. Muller, and M.W. Beukers GPCR structure and activation: an essential role for the first extracellular loop in activating the adenosine A2B receptor FASEB J 25 2011 632 643
    • (2011) FASEB J , vol.25 , pp. 632-643
    • Peeters, M.C.1    Van Westen, G.J.2    Guo, D.3    Wisse, L.E.4    Muller, C.E.5    Beukers, M.W.6
  • 3
    • 79954782236 scopus 로고    scopus 로고
    • Structure of an agonist-bound human A2A adenosine receptor
    • F. Xu, H. Wu, V. Katritch, G.W. Han, K.A. Jacobson, and Z.G. Gao Structure of an agonist-bound human A2A adenosine receptor Science 332 2011 332 337
    • (2011) Science , vol.332 , pp. 332-337
    • Xu, F.1    Wu, H.2    Katritch, V.3    Han, G.W.4    Jacobson, K.A.5    Gao, Z.G.6
  • 4
    • 79955948707 scopus 로고    scopus 로고
    • The structure of the adenosine receptors implications for drug discovery
    • J.R. Lane, V.P. Jaakola, and A.P. Ijzerman The structure of the adenosine receptors implications for drug discovery Adv Pharmacol 61 2011 1 40
    • (2011) Adv Pharmacol , vol.61 , pp. 1-40
    • Lane, J.R.1    Jaakola, V.P.2    Ijzerman, A.P.3
  • 5
    • 78650919353 scopus 로고    scopus 로고
    • Importance of the extracellular loops in G protein-coupled receptors for ligand recognition and receptor activation
    • M.C. Peeters, G.J. van Westen, Q. Li, and A.P. IJzerman Importance of the extracellular loops in G protein-coupled receptors for ligand recognition and receptor activation Trends Pharmacol Sci 32 2011 35 42
    • (2011) Trends Pharmacol Sci , vol.32 , pp. 35-42
    • Peeters, M.C.1    Van Westen, G.J.2    Li, Q.3    Ijzerman, A.P.4
  • 6
    • 79952033865 scopus 로고    scopus 로고
    • International union of basic and clinical pharmacology. LXXXI. Nomenclature and classification of adenosine receptors - An update
    • B.B. Fredholm, A.P. IJzerman, K.A. Jacobson, J. Linden, and C.E. Muller International union of basic and clinical pharmacology. LXXXI. Nomenclature and classification of adenosine receptors - an update Pharmacol Rev 63 2011 1 34
    • (2011) Pharmacol Rev , vol.63 , pp. 1-34
    • Fredholm, B.B.1    Ijzerman, A.P.2    Jacobson, K.A.3    Linden, J.4    Muller, C.E.5
  • 7
    • 0028050692 scopus 로고
    • Role of the second extracellular loop of adenosine receptors in agonist and antagonist binding. Analysis of chimeric A1/A3 adenosine receptors
    • M.E. Olah, K.A. Jacobson, and G.L. Stiles Role of the second extracellular loop of adenosine receptors in agonist and antagonist binding. Analysis of chimeric A1/A3 adenosine receptors J Biol Chem 269 1994 24692 24698
    • (1994) J Biol Chem , vol.269 , pp. 24692-24698
    • Olah, M.E.1    Jacobson, K.A.2    Stiles, G.L.3
  • 9
    • 34548476934 scopus 로고    scopus 로고
    • Critical role for the second extracellular loop in the binding of both orthosteric and allosteric G protein-coupled receptor ligands
    • V.A. Avlani, K.J. Gregory, C.J. Morton, M.W. Parker, P.M. Sexton, and A. Christopoulos Critical role for the second extracellular loop in the binding of both orthosteric and allosteric G protein-coupled receptor ligands J Biol Chem 282 2007 25677 25686
    • (2007) J Biol Chem , vol.282 , pp. 25677-25686
    • Avlani, V.A.1    Gregory, K.J.2    Morton, C.J.3    Parker, M.W.4    Sexton, P.M.5    Christopoulos, A.6
  • 10
    • 77953485027 scopus 로고    scopus 로고
    • Structural determinants of allosteric agonism and modulation at the M4 muscarinic acetylcholine receptor: Identification of ligand-specific and global activation mechanisms
    • V. Nawaratne, K. Leach, C.C. Felder, P.M. Sexton, and A. Christopoulos Structural determinants of allosteric agonism and modulation at the M4 muscarinic acetylcholine receptor: identification of ligand-specific and global activation mechanisms J Biol Chem 285 2010 19012 19021
    • (2010) J Biol Chem , vol.285 , pp. 19012-19021
    • Nawaratne, V.1    Leach, K.2    Felder, C.C.3    Sexton, P.M.4    Christopoulos, A.5
  • 11
    • 33744959047 scopus 로고    scopus 로고
    • Genetic analysis of the first and third extracellular loops of the C5a receptor reveals an essential WXFG motif in the first loop
    • J. Klco, G. Nikiforovich, and T. Baranski Genetic analysis of the first and third extracellular loops of the C5a receptor reveals an essential WXFG motif in the first loop J Biol Chem 281 2006 12010 12019
    • (2006) J Biol Chem , vol.281 , pp. 12010-12019
    • Klco, J.1    Nikiforovich, G.2    Baranski, T.3
  • 12
    • 48749099119 scopus 로고    scopus 로고
    • Evidence for cooperative signal triggering at the extracellular loops of the TSH receptor
    • G. Kleinau, H. Jaeschke, S. Mueller, B.M. Raaka, S. Neumann, and R. Paschke Evidence for cooperative signal triggering at the extracellular loops of the TSH receptor FASEB J 22 2008 2798 2808
    • (2008) FASEB J , vol.22 , pp. 2798-2808
    • Kleinau, G.1    Jaeschke, H.2    Mueller, S.3    Raaka, B.M.4    Neumann, S.5    Paschke, R.6
  • 13
    • 10644247627 scopus 로고    scopus 로고
    • The third extracellular loop of G-protein-coupled receptors: More than just a linker between two important transmembrane helices
    • Z. Lawson, and M. Wheatley The third extracellular loop of G-protein-coupled receptors: more than just a linker between two important transmembrane helices Biochem Soc Trans 32 2004 1048 1050
    • (2004) Biochem Soc Trans , vol.32 , pp. 1048-1050
    • Lawson, Z.1    Wheatley, M.2
  • 14
    • 79959564813 scopus 로고    scopus 로고
    • Agonist-bound adenosine A2A receptor structures reveal common features of GPCR activation
    • G. Lebon, T. Warne, P.C. Edwards, K. Bennett, C.J. Langmead, and A.G. Leslie Agonist-bound adenosine A2A receptor structures reveal common features of GPCR activation Nature 474 2011 521 525
    • (2011) Nature , vol.474 , pp. 521-525
    • Lebon, G.1    Warne, T.2    Edwards, P.C.3    Bennett, K.4    Langmead, C.J.5    Leslie, A.G.6
  • 15
    • 56749103466 scopus 로고    scopus 로고
    • The 2.6 angstrom crystal structure of a human A2A adenosine receptor bound to an antagonist
    • V.P. Jaakola, M.T. Griffith, M.A. Hanson, V. Cherezov, E.Y. Chien, and J.R. Lane The 2.6 angstrom crystal structure of a human A2A adenosine receptor bound to an antagonist Science 322 2008 1211 1217
    • (2008) Science , vol.322 , pp. 1211-1217
    • Jaakola, V.P.1    Griffith, M.T.2    Hanson, M.A.3    Cherezov, V.4    Chien, E.Y.5    Lane, J.R.6
  • 16
    • 0034650702 scopus 로고    scopus 로고
    • Functional coupling of mammalian receptors to the yeast mating pathway using novel yeast/mammalian G protein alpha-subunit chimeras
    • A. Brown, S. Dyos, M. Whiteway, J. White, M. Watson, and M. Marzioch Functional coupling of mammalian receptors to the yeast mating pathway using novel yeast/mammalian G protein alpha-subunit chimeras Yeast 16 2000 11 22
    • (2000) Yeast , vol.16 , pp. 11-22
    • Brown, A.1    Dyos, S.2    Whiteway, M.3    White, J.4    Watson, M.5    Marzioch, M.6
  • 17
    • 1342329641 scopus 로고    scopus 로고
    • Random mutagenesis of the human adenosine A2B receptor followed by growth selection in yeast. Identification of constitutively active and gain of function mutations
    • M. Beukers, J. van Oppenraaij, P. van der Hoorn, C. Blad, H. den Dulk, and J. Brouwer Random mutagenesis of the human adenosine A2B receptor followed by growth selection in yeast. Identification of constitutively active and gain of function mutations Mol Pharmacol 65 2004 702 710
    • (2004) Mol Pharmacol , vol.65 , pp. 702-710
    • Beukers, M.1    Van Oppenraaij, J.2    Van Der Hoorn, P.3    Blad, C.4    Den Dulk, H.5    Brouwer, J.6
  • 18
    • 70349336867 scopus 로고    scopus 로고
    • Determination of adenosine A1 receptor agonist and antagonist pharmacology using Saccharomyces cerevisiae: Implications for ligand screening and functional selectivity
    • G.D. Stewart, C. Valant, S.J. Dowell, D. Mijaljica, R.J. Devenish, and P.J. Scammells Determination of adenosine A1 receptor agonist and antagonist pharmacology using Saccharomyces cerevisiae: implications for ligand screening and functional selectivity J Pharmacol Exp Ther 331 2009 277 286
    • (2009) J Pharmacol Exp Ther , vol.331 , pp. 277-286
    • Stewart, G.D.1    Valant, C.2    Dowell, S.J.3    Mijaljica, D.4    Devenish, R.J.5    Scammells, P.J.6
  • 19
    • 18744402177 scopus 로고    scopus 로고
    • Essential role for the second extracellular loop in C5a receptor activation
    • J. Klco, C. Wiegand, K. Narzinski, and T. Baranski Essential role for the second extracellular loop in C5a receptor activation Nat Struct Mol Biol 12 2005 320 326
    • (2005) Nat Struct Mol Biol , vol.12 , pp. 320-326
    • Klco, J.1    Wiegand, C.2    Narzinski, K.3    Baranski, T.4
  • 20
    • 18744411809 scopus 로고    scopus 로고
    • The second extracellular loop: A damper for G protein-coupled receptors
    • D. Massotte, and B.L. Kieffer The second extracellular loop: a damper for G protein-coupled receptors Nat Struct Mol Biol 12 2005 287 288
    • (2005) Nat Struct Mol Biol , vol.12 , pp. 287-288
    • Massotte, D.1    Kieffer, B.L.2
  • 21
    • 0026562884 scopus 로고
    • Improved method for high efficiency transformation of intact yeast cells
    • D. Gietz, A. St Jean, R.A. Woods, and R.H. Schiestl Improved method for high efficiency transformation of intact yeast cells Nucleic Acids Res 20 1992 1425
    • (1992) Nucleic Acids Res , vol.20 , pp. 1425
    • Gietz, D.1    St Jean, A.2    Woods, R.A.3    Schiestl, R.H.4
  • 22
    • 0033577779 scopus 로고    scopus 로고
    • A constitutively active G-protein-coupled receptor causes mating self-compatibility in the mushroom Coprinus
    • N.S. Olesnicky, A.J. Brown, S.J. Dowell, and L.A. Casselton A constitutively active G-protein-coupled receptor causes mating self-compatibility in the mushroom Coprinus EMBO J 18 1999 2756 2763
    • (1999) EMBO J , vol.18 , pp. 2756-2763
    • Olesnicky, N.S.1    Brown, A.J.2    Dowell, S.J.3    Casselton, L.A.4
  • 23
    • 0034623005 scopus 로고    scopus 로고
    • T-Coffee. A novel method for fast and accurate multiple sequence alignment
    • C. Notredame, D.G. Higgins, and J. Heringa T-Coffee. A novel method for fast and accurate multiple sequence alignment J Mol Biol 302 2000 205 217
    • (2000) J Mol Biol , vol.302 , pp. 205-217
    • Notredame, C.1    Higgins, D.G.2    Heringa, J.3
  • 25
    • 0034578519 scopus 로고    scopus 로고
    • Serine and alanine mutagenesis of the nine native cysteine residues of the human A(1) adenosine receptor
    • D.J. Scholl, and J.N. Wells Serine and alanine mutagenesis of the nine native cysteine residues of the human A(1) adenosine receptor Biochem Pharmacol 60 2000 1647 1654
    • (2000) Biochem Pharmacol , vol.60 , pp. 1647-1654
    • Scholl, D.J.1    Wells, J.N.2
  • 26
    • 0030614454 scopus 로고    scopus 로고
    • Identification of A2a adenosine receptor domains involved in selective coupling to Gs. Analysis of chimeric A1/A2a adenosine receptors
    • M.E. Olah Identification of A2a adenosine receptor domains involved in selective coupling to Gs. Analysis of chimeric A1/A2a adenosine receptors J Biol Chem 272 1997 337 344
    • (1997) J Biol Chem , vol.272 , pp. 337-344
    • Olah, M.E.1
  • 28
    • 33749993417 scopus 로고    scopus 로고
    • The consensus coding sequences of human breast and colorectal cancers
    • T. Sjoblom, S. Jones, L.D. Wood, D.W. Parsons, J. Lin, and T.D. Barber The consensus coding sequences of human breast and colorectal cancers Science 314 2006 268 274
    • (2006) Science , vol.314 , pp. 268-274
    • Sjoblom, T.1    Jones, S.2    Wood, L.D.3    Parsons, D.W.4    Lin, J.5    Barber, T.D.6
  • 29
    • 0028950255 scopus 로고
    • The two-state model of receptor activation
    • P. Leff The two-state model of receptor activation Trends Pharmacol Sci 16 1995 89 97
    • (1995) Trends Pharmacol Sci , vol.16 , pp. 89-97
    • Leff, P.1
  • 30
    • 77958039571 scopus 로고    scopus 로고
    • Energy landscapes as a tool to integrate GPCR structure, dynamics, and function
    • X. Deupi, and B.K. Kobilka Energy landscapes as a tool to integrate GPCR structure, dynamics, and function Physiology (Bethesda) 25 2010 293 303
    • (2010) Physiology (Bethesda) , vol.25 , pp. 293-303
    • Deupi, X.1    Kobilka, B.K.2
  • 31
    • 36349016730 scopus 로고    scopus 로고
    • Roof and floor of the muscarinic binding pocket: Variations in the binding modes of orthosteric ligands
    • J.A. Goodwin, E.C. Hulme, C.J. Langmead, and B.G. Tehan Roof and floor of the muscarinic binding pocket: variations in the binding modes of orthosteric ligands Mol Pharmacol 72 2007 1484 1496
    • (2007) Mol Pharmacol , vol.72 , pp. 1484-1496
    • Goodwin, J.A.1    Hulme, E.C.2    Langmead, C.J.3    Tehan, B.G.4
  • 32
    • 0030066317 scopus 로고    scopus 로고
    • Thrombin receptor activating mutations. Alteration of an extracellular agonist recognition domain causes constitutive signaling
    • T. Nanevicz, L. Wang, M. Chen, M. Ishii, and S.R. Coughlin Thrombin receptor activating mutations. Alteration of an extracellular agonist recognition domain causes constitutive signaling J Biol Chem 271 1996 702 706
    • (1996) J Biol Chem , vol.271 , pp. 702-706
    • Nanevicz, T.1    Wang, L.2    Chen, M.3    Ishii, M.4    Coughlin, S.R.5
  • 33
    • 0042624659 scopus 로고    scopus 로고
    • Opioid receptor random mutagenesis reveals a mechanism for G protein-coupled receptor activation
    • F. Decaillot, K. Befort, D. Filliol, S. Yue, P. Walker, and B. Kieffer Opioid receptor random mutagenesis reveals a mechanism for G protein-coupled receptor activation Nat Struct Biol 10 2003 629 636
    • (2003) Nat Struct Biol , vol.10 , pp. 629-636
    • Decaillot, F.1    Befort, K.2    Filliol, D.3    Yue, S.4    Walker, P.5    Kieffer, B.6
  • 34
    • 0034691035 scopus 로고    scopus 로고
    • Systematic identification of mutations that constitutively activate the angiotensin II type 1A receptor by screening a randomly mutated cDNA library with an original pharmacological bioassay
    • C. Parnot, S. Bardin, S. Miserey-Lenkei, D. Guedin, P. Corvol, and E. Clauser Systematic identification of mutations that constitutively activate the angiotensin II type 1A receptor by screening a randomly mutated cDNA library with an original pharmacological bioassay Proc Natl Acad Sci USA 97 2000 7615 7620
    • (2000) Proc Natl Acad Sci USA , vol.97 , pp. 7615-7620
    • Parnot, C.1    Bardin, S.2    Miserey-Lenkei, S.3    Guedin, D.4    Corvol, P.5    Clauser, E.6
  • 35
    • 34147167536 scopus 로고    scopus 로고
    • Multiple residues in the second extracellular loop are critical for M3 muscarinic acetylcholine receptor activation
    • M. Scarselli, B. Li, S. Kim, and J. Wess Multiple residues in the second extracellular loop are critical for M3 muscarinic acetylcholine receptor activation J Biol Chem 282 2007 7385 7396
    • (2007) J Biol Chem , vol.282 , pp. 7385-7396
    • Scarselli, M.1    Li, B.2    Kim, S.3    Wess, J.4
  • 37
    • 0035209620 scopus 로고    scopus 로고
    • International Union of Pharmacology. XXV. Nomenclature and classification of adenosine receptors
    • B.B. Fredholm, A.P. IJzerman, K.A. Jacobson, K.N. Klotz, and J. Linden International Union of Pharmacology. XXV. Nomenclature and classification of adenosine receptors Pharmacol Rev 53 2001 527 552
    • (2001) Pharmacol Rev , vol.53 , pp. 527-552
    • Fredholm, B.B.1    Ijzerman, A.P.2    Jacobson, K.A.3    Klotz, K.N.4    Linden, J.5
  • 38
    • 78149496159 scopus 로고    scopus 로고
    • Allosteric modulation of G protein-coupled receptors: A pharmacological perspective
    • P. Keov, P.M. Sexton, and A. Christopoulos Allosteric modulation of G protein-coupled receptors: a pharmacological perspective Neuropharmacology 60 2010 24 35
    • (2010) Neuropharmacology , vol.60 , pp. 24-35
    • Keov, P.1    Sexton, P.M.2    Christopoulos, A.3
  • 39
    • 53449093828 scopus 로고    scopus 로고
    • G-protein-coupled receptors: From classical modes of modulation to allosteric mechanisms
    • T.M. Bridges, and C.W. Lindsley G-protein-coupled receptors: from classical modes of modulation to allosteric mechanisms ACS Chem Biol 3 2008 530 541
    • (2008) ACS Chem Biol , vol.3 , pp. 530-541
    • Bridges, T.M.1    Lindsley, C.W.2
  • 40
    • 77954612317 scopus 로고    scopus 로고
    • Allosteric activators of muscarinic receptors as novel approaches for treatment of CNS disorders
    • G.J. Digby, J.K. Shirey, and P.J. Conn Allosteric activators of muscarinic receptors as novel approaches for treatment of CNS disorders Mol Biosyst 6 2010 1345 1354
    • (2010) Mol Biosyst , vol.6 , pp. 1345-1354
    • Digby, G.J.1    Shirey, J.K.2    Conn, P.J.3
  • 41
    • 36849071252 scopus 로고    scopus 로고
    • Allosteric small molecules unveil a role of an extracellular E2/transmembrane helix 7 junction for G protein-coupled receptor activation
    • D. Jager, C. Schmalenbach, S. Prilla, J. Schrobang, A. Kebig, and M. Sennwitz Allosteric small molecules unveil a role of an extracellular E2/transmembrane helix 7 junction for G protein-coupled receptor activation J Biol Chem 282 2007 34968 34976
    • (2007) J Biol Chem , vol.282 , pp. 34968-34976
    • Jager, D.1    Schmalenbach, C.2    Prilla, S.3    Schrobang, J.4    Kebig, A.5    Sennwitz, M.6
  • 43
    • 0029960789 scopus 로고
    • Glutamate residues in the second extracellular loop of the human A2a adenosine receptor are required for ligand recognition
    • J. Kim, Q. Jiang, M. Glashofer, S. Yehle, J. Wess, and K. Jacobson Glutamate residues in the second extracellular loop of the human A2a adenosine receptor are required for ligand recognition Mol Pharmacol 49 1995 683 691
    • (1995) Mol Pharmacol , vol.49 , pp. 683-691
    • Kim, J.1    Jiang, Q.2    Glashofer, M.3    Yehle, S.4    Wess, J.5    Jacobson, K.6
  • 44
    • 7444262496 scopus 로고    scopus 로고
    • The status, quality, and expansion of the NIH full-length cDNA project: The Mammalian Gene Collection (MGC)
    • D.S. Gerhard, L. Wagner, E.A. Feingold, C.M. Shenmen, L.H. Grouse, and G. Schuler The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC) Genome Res 14 2004 2121 2127
    • (2004) Genome Res , vol.14 , pp. 2121-2127
    • Gerhard, D.S.1    Wagner, L.2    Feingold, E.A.3    Shenmen, C.M.4    Grouse, L.H.5    Schuler, G.6


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.