REFERENCES
- Hulme E C, Birdsall N J, Buckley N J. Muscarinic receptor subtypes. Annu Rev Pharmacol Toxicol 1990; 30: 633–673, [PUBMED], [INFOTRIEVE], [CSA]
- Jakubik J, Bacakova L, el-Fakahany E E, Tucek S. Constitutive activity of the M1-M4 subtypes of muscarinic receptors in transfected CHO cells and of muscarinic receptors in the heart cells revealed by negative antagonists. FEBS Lett. 1995; 377: 275–279, [PUBMED], [INFOTRIEVE], [CSA], [CROSSREF]
- Migeon J C, Nathanson N M. Differential regulation of cAMP-mediated gene transcription by M1 and M4 muscarinic acetylcholine receptors. Preferential coupling of M4 receptors to Gi alpha-2. J Biol Chem 1994; 269: 9767–9773, [PUBMED], [INFOTRIEVE], [CSA]
- Ashkenazi A, Winslow J W, Peralta E G, Peterson G L, Schimerlik M I, Capon D J, Ramachandran J. An M2 muscarinic receptor subtype coupled to both adenylyl cyclase and phosphoinositide turnover. Science 1987; 238: 672–675, [PUBMED], [INFOTRIEVE], [CSA]
- Peralta E G, Ashkenazi A, Winslow J W, Ramachandran J, Capon D J. Differential regulation of PI hydrolysis and adenylyl cyclase by muscarinic receptor subtypes. Nature 1988; 334: 434–437, [PUBMED], [INFOTRIEVE], [CSA], [CROSSREF]
- Conklin B R, Brann M R, Buckley N J, Ma A L, Bonner T I, Axelrod J. Stimulation of arachidonic acid release and inhibition of mitogenesis by cloned genes for muscarinic receptor subtypes stably expressed in A9 L cells. Proc Natl Acad Sci USA 1988; 85: 8698–8702, [PUBMED], [INFOTRIEVE], [CSA]
- Jones S V, Heilman C J, Brann M R. Functional responses of cloned muscarinic receptors expressed in CHO-K1 cells. Mol Pharmacol 1991; 40: 242–247, [PUBMED], [INFOTRIEVE], [CSA]
- Felder C C, Kanterman R Y, Ma A L, Axelrod J. A transfected M1 muscarinic acetylcholine receptor stimulates adenylate cyclase via phosphatidylinositol hydrolysis. J Biol Chem 1989; 264: 20356–20362, [PUBMED], [INFOTRIEVE], [CSA]
- Vogel W K, Mosser V A, Bulseco D A, Schimerlik M I. Porcine m2 muscarinic acetylcholine receptor-effector coupling in Chinese hamster ovary cells. J Biol Chem. 1995; 270: 15485–15493, [PUBMED], [INFOTRIEVE], [CSA], [CROSSREF]
- Giles W, Noble S J. Changes in membrane currents in bullfrog atrium produced by acetylcholine. J Physiol 1976; 261: 103–123, [PUBMED], [INFOTRIEVE], [CSA]
- Soejima M, Noma A. Mode of regulation of the ACh-sensitive K-channel by the muscarinic receptor in rabbit atrial cells. Pflugers Arch 1984; 400: 424–431, [PUBMED], [INFOTRIEVE], [CSA], [CROSSREF]
- Hanf R, Li Y, Szabo G, Fischmeister R. Agonist-independent effects of muscarinic antagonists on Ca2+ and K+ currents in frog and rat cardiac cells. J Physiol 1993; 461: 743–765, [PUBMED], [INFOTRIEVE], [CSA]
- Peter J C, Wallukat G, Tugler J, Maurice D, Roegel J C, Briand J P, Hoebeke J. Modulation of the M2 muscarinic acetylcholine receptor activity with monoclonal anti-M2 receptor antibody fragments. J Biol Chem 2004; 279: 55697–55706, [PUBMED], [INFOTRIEVE], [CSA], [CROSSREF]
- Hilf G, Jakobs K H. Agonist-independent inhibition of G protein activation by muscarinic acetylcholine receptor antagonists in cardiac membranes. Eur J Pharmacol 1992; 225: 245–252, [PUBMED], [INFOTRIEVE], [CSA], [CROSSREF]
- Ricny J, Gualtieri F, Tucek S. Constitutive inhibitory action of muscarinic receptors on adenylyl cyclase in cardiac membranes and its stereospecific suppression by hyoscyamine. Physiol Res 2002; 51: 131–137, [PUBMED], [INFOTRIEVE], [CSA]
- Matesic D F, Luthin G R. Atropine dissociates complexes of muscarinic acetylcholine receptor and guanine nucleotide-binding protein in heart membranes. FEBS Lett 1991; 284: 184–186, [PUBMED], [INFOTRIEVE], [CSA], [CROSSREF]
- Berrie C P, Birdsall N J, Burgen A S, Hulme E C. Guanine nucleotides modulate muscarinic receptor binding in the heart. Biochem Biophys Res Commun 1979; 87: 1000–1005, [PUBMED], [INFOTRIEVE], [CSA], [CROSSREF]
- Burgisser E, De Lean A, Lefkowitz R J. Reciprocal modulation of agonist and antagonist binding to muscarinic cholinergic receptor by guanine nucleotide. Proc Natl Acad Sci USA 1982; 79: 1732–1736, [PUBMED], [INFOTRIEVE], [CSA]
- Hosey M M. Regulation of antagonist binding to cardiac muscarinic receptors. Biochem Biophys Res Commun 1982; 107: 314–321, [PUBMED], [INFOTRIEVE], [CSA], [CROSSREF]
- Wang H, Han H, Zhang L, Shi H, Schram G, Nattel S, Wang Z. Expression of multiple subtypes of muscarinic receptors and cellular distribution in the human heart. Mol Pharmacol 2001; 59: 1029–1036, [PUBMED], [INFOTRIEVE], [CSA]
- Chidiac P, Hebert T E, Valiquette M, Dennis M, Bouvier M. Inverse agonist activity of beta-adrenergic antagonists. Mol Pharmacol 1994; 45: 490–499, [PUBMED], [INFOTRIEVE], [CSA]
- Ford D J, Essex A, Spalding T A, Burstein E S, Ellis J. Homologous mutations near the junction of the sixth transmembrane domain and the third extracellular loop lead to constitutive activity and enhanced agonist affinity at all muscarinic receptor subtypes. J Pharmacol Exp Ther 2002; 300: 810–817, [PUBMED], [INFOTRIEVE], [CSA], [CROSSREF]
- Brauner-Osborne H, Brann M R. Pharmacology of muscarinic acetylcholine receptor subtypes (m1-m5): High throughput assays in mammalian cells. Eur J Pharmacol 1996; 295: 93–102, [PUBMED], [INFOTRIEVE], [CSA], [CROSSREF]
- Burstein E S, Spalding T A, Brann M R. The second intracellular loop of the M5 muscarinic receptor is the switch which enables G-protein coupling. J Biol Chem 1998b; 273: 24322–24327, [PUBMED], [INFOTRIEVE], [CSA], [CROSSREF]
- Spalding T A, Burstein E S, Wells J W, Brann M R. Constitutive activation of the M5 muscarinic receptor by a series of mutations at the extracellular end of transmembrane 6. Biochemistry 1997; 36: 10109–10116, [PUBMED], [INFOTRIEVE], [CSA], [CROSSREF]
- Spalding T A, Burstein E S, Henderson S C, Ducote K R, Brann M R. Identification of a ligand-dependent switch within a muscarinic receptor. J Biol Chem 1998; 273: 21563–21568, [PUBMED], [INFOTRIEVE], [CSA], [CROSSREF]
- Conklin B R, Farfel Z, Lustig K D, Julius D, Bourne H R. Substitution of three amino acids switches receptor specificity of Gq alpha to that of Gi alpha. Nature 1993; 363: 274–276, [PUBMED], [INFOTRIEVE], [CSA], [CROSSREF]
- Burstein E S, Spalding T A, Brauner-Osborne H, Brann M R. Constitutive activation of muscarinic receptors by the G-protein Gq. FEBS Lett 1995a; 363: 261–263, [PUBMED], [INFOTRIEVE], [CSA], [CROSSREF]
- Burstein E S, Spalding T A, Hill-Eubanks D, Brann M R. Structure-function of muscarinic receptor coupling to G proteins. Random saturation mutagenesis identifies a critical determinant of receptor affinity for G proteins. J Biol Chem 1995b; 270: 3141–3146, [PUBMED], [INFOTRIEVE], [CSA], [CROSSREF]
- Burstein E S, Spalding T A, Brann M R. Pharmacology of muscarinic receptor subtypes constitutively activated by G proteins. Mol Pharmacol 1997a; 51: 312–319, [PUBMED], [INFOTRIEVE], [CSA]
- Burstein E S, Brauner-Osborne H, Spalding T A, Conklin B R, Brann M R. Interactions of muscarinic receptors with the heterotrimeric G proteins Gq and G12: Transduction of proliferative signals. J Neurochem 1997b; 68: 525–533, [PUBMED], [INFOTRIEVE], [CSA]
- Uustare A, Nasman J, Akerman K E, Rinken A. Characterization of M2 muscarinic receptor activation of different G protein subtypes. Neurochem Int 2004; 44: 119–124, [PUBMED], [INFOTRIEVE], [CSA], [CROSSREF]
- Costa T, Herz A. Antagonists with negative intrinsic activity at delta opioid receptors coupled to GTP-binding proteins. Proc Natl Acad Sci USA 1989; 86: 7321–7325, [PUBMED], [INFOTRIEVE], [CSA]
- Kenakin T. Principles: Receptor theory in pharmacology. Trends Pharmacol Sci 2004; 25: 186–192, [PUBMED], [INFOTRIEVE], [CSA], [CROSSREF]
- Samama P, Cotecchia S, Costa T, Lefkowitz R J. A mutation-induced activated state of the beta 2 adrenergic receptor. Extending the ternary complex model. J Biol Chem 1993; 268: 4625–4636, [PUBMED], [INFOTRIEVE], [CSA]
- Leff P. The two-state model of receptor activation. Trends Pharmacol Sci 1995; 16: 89–97, [PUBMED], [INFOTRIEVE], [CSA], [CROSSREF]
- Weiss J M, Morgan P H, Lutz M W, Kenakin T P. The cubic ternary complex receptor–occupancy model I. Model description. J Theor Biol 1996; 178: 151–167, [CSA], [CROSSREF]
- Alves I D, Salamon Z, Varga E, Yamamura H I, Tollin G, Hruby V J. Direct observation of G-protein binding to the human delta-opioid receptor using plasmon-waveguide resonance spectroscopy. J Biol Chem 2003; 278: 48890–48897, [PUBMED], [INFOTRIEVE], [CSA], [CROSSREF]
- De Lean A, Stadel J M, Lefkowitz R J. A ternary complex model explains the agonist-specific binding properties of the adenylate cyclase-coupled beta-adrenergic receptor. J Biol Chem 1980; 255: 7108–7117, [PUBMED], [INFOTRIEVE], [CSA]
- Burstein E S, Piu F, Ma J, Weissman J T, Currier E A, Nash N R, Schiffer H H, Del Tredici A L, Brann M R. Integrative functional assays, chemical genomics and high throughput screening: Harnessing signal transduction pathways to a common HTS readout. Curr Pharm Design, In press
- Kenakin T. Related pharmacological proteus?. Trends Pharmacol Sci 1995; 16: 256–258, [PUBMED], [INFOTRIEVE], [CSA], [CROSSREF]
- Kenakin T. Inverse, protean, and ligand-selective agonism: Matters of receptor conformation. FASEB J 2001; 15: 598–611, [PUBMED], [INFOTRIEVE], [CSA], [CROSSREF]
- Kenakin T. Ligand-selective receptor conformations revisited: The promise and the problem. Trends Pharmacol Sci 2003; 24: 346–354, [PUBMED], [INFOTRIEVE], [CSA], [CROSSREF]
- Kenakin T, Onaran O. The ligand paradox between affinity and efficacy: Can you be there and not make a difference?. Trends Pharmacol Sci 2002; 23: 275–280, [PUBMED], [INFOTRIEVE], [CSA], [CROSSREF]
- Park P S, Sum C S, Pawagi A B, Wells J W. Cooperativity and oligomeric status of cardiac muscarinic cholinergic receptors. Biochemistry 2002; 41: 5588–5604, [PUBMED], [INFOTRIEVE], [CSA], [CROSSREF]
- Park P S, Filipek S, Wells J W, Palczewski K. Oligomerization of G protein-coupled receptors: Past, present, and future. Biochemistry 2004; 43: 15643–15656, [PUBMED], [INFOTRIEVE], [CSA], [CROSSREF]
- Zeng F Y, Wess J. Identification and molecular characterization of m3 muscarinic receptor dimers. J Biol Chem 1999; 274: 19487–19497, [PUBMED], [INFOTRIEVE], [CSA], [CROSSREF]
- Palczewski K, Kumasaka T, Hori T, Behnke C A, Motoshima H, Fox B A, Trong I, Teller D C, Okada T, Stenkamp R E, Yamamoto M, Miyano M. Crystal structure of rhodopsin: A G protein-coupled receptor. Science 2000; 289: 739–745, [PUBMED], [INFOTRIEVE], [CSA], [CROSSREF]
- Hulme E C, Lu Z L, Bee M S. Scanning mutagenesis studies of the M1 muscarinic acetylcholine receptor. Receptors Channels 2003; 9: 215–228, [PUBMED], [INFOTRIEVE], [CSA], [CROSSREF]
- Fraser C M, Wang C D, Robinson D A, Gocayne J D, Venter J C. Site-directed mutagenesis of m1 muscarinic acetylcholine receptors: Conserved aspartic acids play important roles in receptor function. Mol Pharmacol 1989; 36: 840–847, [PUBMED], [INFOTRIEVE], [CSA]
- Spalding T A, Birdsall N J, Curtis C A, Hulme E C. Acetylcholine mustard labels the binding site aspartate in muscarinic acetylcholine receptors. J Biol Chem 1994; 269: 4092–4097, [PUBMED], [INFOTRIEVE], [CSA]
- Page K M, Curtis C A, Jones P G, Hulme E C. The functional role of the binding site aspartate in muscarinic acetylcholine receptors, probed by site-directed mutagenesis. Eur J Pharmacol 1995; 289: 429–437, [PUBMED], [INFOTRIEVE], [CSA]
- Wess J, Gdula D, Brann M R. Site-directed mutagenesis of the M3 muscarinic receptor: Identification of a series of threonine and tyrosine residues involved in agonist but not antagonist binding. EMBO J 1991; 10: 3729–3734, [PUBMED], [INFOTRIEVE], [CSA]
- Wess J, Maggio R, Palmer J R, Vogel Z. Role of conserved threonine and tyrosine residues in acetylcholine binding and muscarinic receptor activation. A study with M3 muscarinic receptor point mutants. J Biol Chem 1992; 267: 19313–19319, [PUBMED], [INFOTRIEVE], [CSA]
- Bluml K, Mutschler E, Wess J. Functional role in ligand binding and receptor activation of an asparagine residue present in the sixth transmembrane domain of all muscarinic acetylcholine receptors. J Biol Chem 1994; 269: 18870–18876, [PUBMED], [INFOTRIEVE], [CSA]
- Ward S D, Curtis C A, Hulme E C. Alanine-scanning mutagenesis of transmembrane domain 6 of the M(1) muscarinic acetylcholine receptor suggests that Tyr381 plays key roles in receptor function. Mol Pharmacol 1999; 56: 1031–1041, [PUBMED], [INFOTRIEVE], [CSA]
- Jensen A A, Spalding T A. Allosteric modulation of G-protein coupled receptors. Eur J Pharm Sci 2004; 21: 407–420, [PUBMED], [INFOTRIEVE], [CSA], [CROSSREF]
- Spalding T A, Trotter C, Skjaerbaek N, Messier T L, Currier E A, Burstein E S, Li D, Hacksell U, Brann M R. Discovery of an ectopic activation site on the M(1) muscarinic receptor. Mol Pharmacol 2002; 61: 1297–1302, [PUBMED], [INFOTRIEVE], [CSA], [CROSSREF]
- Sur C, Mallorga P J, Wittmann M, Jacobson M A, Pascarella D, Williams J B, Brandish P E, Pettibone D J, Scolnick E M, Conn P J. N-desmethylclozapine, an allosteric agonist at muscarinic 1 receptor, potentiates N-methyl-D-aspartate receptor activity. Proc Natl Acad Sci USA 2003; 100: 13674–13679, [PUBMED], [INFOTRIEVE], [CSA], [CROSSREF]
- Ballesteros J A, Weinstein H. Integrated methods for modeling G-protein coupled receptors. Methods Neurosci 1995; 25: 366–428, [CSA]
- Stockton J M, Birdsall N J, Burgen A S, Hulme E C. Modification of the binding properties of muscarinic receptors by gallamine. Mol Pharmacol 1983; 23: 551–557, [PUBMED], [INFOTRIEVE], [CSA]
- Tucek S, Musilkova J, Nedoma J, Proska J, Shelkovnikov S, Vorlicek J. Positive cooperativity in the binding of alcuronium and N-methylscopolamine to muscarinic acetylcholine receptors. Mol Pharmacol 1990; 38: 674–680, [PUBMED], [INFOTRIEVE], [CSA]
- Gnagey A L, Seidenberg M, Ellis J. Site-directed mutagenesis reveals two epitopes involved in the subtype selectivity of the allosteric interactions of gallamine at muscarinic acetylcholine receptors. Mol Pharmacol 1999; 56: 1245–1253, [PUBMED], [INFOTRIEVE], [CSA]
- Matsui H, Lazareno S, Birdsall N J. Probing of the location of the allosteric site on m1 muscarinic receptors by site-directed mutagenesis. Mol Pharmacol 1995; 47: 88–98, [PUBMED], [INFOTRIEVE], [CSA]
- Lazareno S, Popham A, Birdsall N J. Analogs of WIN 62,577 define a second allosteric site on muscarinic receptors. Mol Pharmacol 2002; 62: 1492–1505, [PUBMED], [INFOTRIEVE], [CSA], [CROSSREF]
- Wess J, Brann M R, Bonner T I. Identification of a small intracellular region of the muscarinic M3 receptor as a determinant of selective coupling to PI turnover. FEBS Lett 1989; 258: 133–136, [PUBMED], [INFOTRIEVE], [CSA], [CROSSREF]
- Wess J, Bonner T I, Dorje F, Brann M R. Delineation of muscarinic receptor domains conferring selectivity of coupling to guanine nucleotide-binding proteins and second messengers. Mol Pharmacol 1990; 38: 517–523, [PUBMED], [CSA]
- Jones P G, Curtis C A, Hulme E C. The function of a highly-conserved arginine residue in activation of the muscarinic M1 receptor. Eur J Pharmacol 1995; 288: 251–257, [PUBMED], [INFOTRIEVE], [CSA], [CROSSREF]
- Hill-Eubanks D, Burstein E S, Spalding T A, Brauner-Osborne H, Brann M R. Structure of a G-protein-coupling domain of a muscarinic receptor predicted by random saturation mutagenesis. J Biol Chem 1996; 271: 3058–3065, [PUBMED], [INFOTRIEVE], [CSA], [CROSSREF]
- Huang X P, Williams F E, Peseckis S M, Messer W S, Jr. Differential modulation of agonist potency and receptor coupling by mutations of Ser388Tyr and Thr389Pro at the junction of transmembrane domain VI and the third extracellular loop of human M(1) muscarinic acetylcholine receptors. Mol Pharmacol 1999; 56: 775–783, [PUBMED], [INFOTRIEVE], [CSA]
- Spalding T A, Burstein E S, Brauner-Osborne H, Hill-Eubanks D, Brann M R. Pharmacology of a constitutively active muscarinic receptor generated by random mutagenesis. J Pharmacol Exp Ther 1995; 275: 1274–1279, [PUBMED], [INFOTRIEVE], [CSA]
- Huang X P, Williams F E, Peseckis S M, Messer W S, Jr. Pharmacological characterization of human M1 muscarinic acetylcholine receptors with double mutations at the junction of TM VI and the third extracellular domain. J Pharmacol Exp Ther 1998; 286: 1129–1139, [PUBMED], [INFOTRIEVE], [CSA]
- Lu Z L, Saldanha J W, Hulme E C. Transmembrane domains 4 and 7 of the M(1) muscarinic acetylcholine receptor are critical for ligand binding and the receptor activation switch. J Biol Chem 2001; 276: 34098–34104, [PUBMED], [INFOTRIEVE], [CSA], [CROSSREF]
- Allman K, Page K M, Curtis C A, Hulme E C. Scanning mutagenesis identifies amino acid side chains in transmembrane domain 5 of the M(1) muscarinic receptor that participate in binding the acetyl methyl group of acetylcholine. Mol Pharmacol 2000; 58: 175–184, [PUBMED], [INFOTRIEVE], [CSA]
- Baldwin J M, Schertler G F, Unger V M. An alpha-carbon template for the transmembrane helices in the rhodopsin family of G-protein-coupled receptors. J Mol Biol 1997; 272: 144–164, [PUBMED], [INFOTRIEVE], [CSA], [CROSSREF]
- Lu Z L, Hulme E C. The functional topography of transmembrane domain 3 of the M1 muscarinic acetylcholine receptor, revealed by scanning mutagenesis. J Biol Chem 1999; 274: 7309–7315, [PUBMED], [INFOTRIEVE], [CSA], [CROSSREF]
- Lu Z L, Hulme E C. A network of conserved intramolecular contacts defines the off-state of the transmembrane switch mechanism in a seven-transmembrane receptor. J Biol Chem 2000; 275: 5682–5686, [PUBMED], [INFOTRIEVE], [CSA], [CROSSREF]
- Bee M S. Doctoral thesis, University College, London 2002
- Wess J, Nanavati S, Vogel Z, Maggio R. Functional role of proline and tryptophan residues highly conserved among G protein-coupled receptors studied by mutational analysis of the M3 muscarinic receptor. EMBO J 1993; 12: 331–338, [PUBMED], [INFOTRIEVE], [CSA]
- Allen L F, Lefkowitz R J, Caron M G, Cotecchia S. G-protein-coupled receptor genes as protooncogenes: Constitutively activating mutation of the alpha 1B-adrenergic receptor enhances mitogenesis and tumorigenicity. Proc Natl Acad Sci USA 1991; 88: 11354–11358, [PUBMED], [INFOTRIEVE], [CSA]
- Kjelsberg M A, Cotecchia S, Ostrowski J, Caron M G, Lefkowitz R J. Constitutive activation of the alpha 1B-adrenergic receptor by all amino acid substitutions at a single site. Evidence for a region which constrains receptor activation. J Biol Chem 1992; 267: 1430–1433, [PUBMED], [INFOTRIEVE], [CSA]
- Hogger P, Shockley M S, Lameh J, Sadee W. Activating and inactivating mutations in N- and C-terminal i3 loop junctions of muscarinic acetylcholine HM1 receptors. J Biol Chem 1995; 270: 7405–7410, [PUBMED], [INFOTRIEVE], [CSA], [CROSSREF]
- Liu J, Blin N, Conklin B R, Wess J. Molecular mechanisms involved in muscarinic acetylcholine receptor-mediated G protein activation studied by insertion mutagenesis. J Biol Chem 1996; 271: 6172–6178, [PUBMED], [INFOTRIEVE], [CSA], [CROSSREF]
- Burstein E S, Spalding T A, Brann M R. Constitutive activation of chimeric m2/m5 muscarinic receptors and delineation of G-protein coupling selectivity domains. Biochem Pharmacol 1996a; 51: 539–544, [PUBMED], [INFOTRIEVE], [CSA], [CROSSREF]
- Burstein E S, Spalding T A, Brann M R. Amino acid side chains that define muscarinic receptor/G-protein coupling. Studies of the third intracellular loop. J Biol Chem 1996b; 271: 2882–2885, [PUBMED], [INFOTRIEVE], [CSA], [CROSSREF]
- Lu Z L, Curtis C A, Jones P G, Pavia J, Hulme E C. The role of the aspartate-arginine-tyrosine triad in the M1 muscarinic receptor: Mutations of aspartate 122 and tyrosine 124 decrease receptor expression but do not abolish signaling. Mol Pharmacol 1997; 51: 234–241, [PUBMED], [INFOTRIEVE], [CSA]
- Spalding T A, Burstein E S. Constitutively active muscarinic receptors. Life Sci 2001; 68: 2511–2516, [PUBMED], [INFOTRIEVE], [CSA], [CROSSREF]
- Baranski T J, Herzmark P, Lichtarge O, Gerber B O, Trueheart J, Meng E C, Iiri T, Sheikh S P, Bourne H R. C5a receptor activation. Genetic identification of critical residues in four transmembrane helices. J Biol Chem 1999; 274: 15757–15765, [PUBMED], [INFOTRIEVE], [CSA], [CROSSREF]
- Geva A, Lassere T B, Lichtarge O, Pollitt S K, Baranski T J. Genetic mapping of the human C5a receptor. Identification of transmembrane amino acids critical for receptor function. J Biol Chem 2000; 275: 35393–353401, [PUBMED], [INFOTRIEVE], [CSA], [CROSSREF]
- Han S J, Hamdan F F, Kim S K, Jacobson K A, Brichta L, Bloodworth L M, Li J H, Wess J. Pronounced conformational changes following agonist activation of the M3 muscarinic acetylcholine receptor. J Biol Chem 2005; 280: 24870–24879, [PUBMED], [INFOTRIEVE], [CSA], [CROSSREF]
- Gether U, Lin S, Ghanouni P, Ballesteros J A, Weinstein H, Kobilka B K. Agonists induce conformational changes in transmembrane domains III and VI of the beta2 adrenoceptor. EMBO J 1997; 16: 6737–6747, [PUBMED], [INFOTRIEVE], [CSA], [CROSSREF]
- Ghanouni P, Steenhuis J J, Farrens D L, Kobilka B K. Agonist-induced conformational changes in the G-protein-coupling domain of the beta 2 adrenergic receptor. Proc Natl Acad Sci USA 2001; 98: 5997–6002, [PUBMED], [INFOTRIEVE], [CSA], [CROSSREF]
- Rasmussen S G, Jensen A D, Liapakis G, Ghanouni P, Javitch J A, Gether U. Mutation of a highly conserved aspartic acid in the beta2 adrenergic receptor: Constitutive activation, structural instability, and conformational rearrangement of transmembrane segment 6. Mol Pharmacol 1999; 56: 175–184, [PUBMED], [INFOTRIEVE], [CSA]
- Sheikh S P, Zvyaga T A, Lichtarge O, Sakmar T P, Bourne H R. Rhodopsin activation blocked by metal-ion-binding sites linking transmembrane helices C and F. Nature 1996; 383: 347–350, [PUBMED], [INFOTRIEVE], [CSA], [CROSSREF]
- Farrens D L, Altenbach C, Yang K, Hubbell W L, Khorana H G. Requirement of rigid-body motion of transmembrane helices for light activation of rhodopsin. Science 1996; 274: 768–770, [PUBMED], [INFOTRIEVE], [CSA], [CROSSREF]
- Dunham T D, Farrens D L. Conformational changes in rhodopsin. Movement of helix f detected by site-specific chemical labeling and fluorescence spectroscopy. J Biol Chem 1999; 274: 1683–1690, [PUBMED], [INFOTRIEVE], [CSA], [CROSSREF]
- Heller Brown J, Taylor P. Muscarinic receptor agonists and antagonists. Goodman and Gilman's The Pharmacological Basis of Therapeutics, 10th ed, J G Hardman, L E Limbird, A G Gilman. McGraw Hill, New York 2002
- Bymaster F P, McKinzie D L, Felder C C, Wess J. Use of M1-M5 muscarinic receptor knockout mice as novel tools to delineate the physiological roles of the muscarinic cholinergic system. Neurochem Res 2003; 28: 437–442, [PUBMED], [INFOTRIEVE], [CSA], [CROSSREF]
- Wess J. Muscarinic acetylcholine receptor knockout mice: Novel phenotypes and clinical implications. Annu Rev Pharmacol Toxicol 2004; 44: 423–450, [PUBMED], [INFOTRIEVE], [CSA], [CROSSREF]
- Wess J, Duttaroy A, Zhang W, Gomeza J, Cui Y, Miyakawa T, Bymaster F P, McKinzie L, Felder C C, Lamping K G, Faraci F M, Deng C, Yamada M. M1-M5 muscarinic receptor knockout mice as novel tools to study the physiological roles of the muscarinic cholinergic system. Receptors Channels 2003; 9: 279–290, [PUBMED], [INFOTRIEVE], [CSA], [CROSSREF]
- Gainetdinov R R, Caron M G. Delineating muscarinic receptor functions. Proc Natl Acad Sci USA 1999; 96: 12222–12223, [PUBMED], [INFOTRIEVE], [CSA], [CROSSREF]
- Gomeza J, Shannon H, Kostenis E, Felder C, Zhang L, Brodkin J, Grinberg A, Sheng H, Wess J. Pronounced pharmacologic deficits in M2 muscarinic acetylcholine receptor knockout mice. Proc Natl Acad Sci USA 1999a; 96: 1692–1697, [PUBMED], [INFOTRIEVE], [CSA], [CROSSREF]
- Matsui M, Griffin M T, Shehnaz D, Taketo M M, Ehlert F J. Increased relaxant action of forskolin and isoproterenol against muscarinic agonist-induced contractions in smooth muscle from M2 receptor knockout mice. J Pharmacol Exp Ther 2003; 305: 106–113, [PUBMED], [INFOTRIEVE], [CSA], [CROSSREF]
- Gerber D J, Sotnikova T D, Gainetdinov R R, Huang S Y, Caron M G, Tonegawa S. Hyperactivity, elevated dopaminergic transmission, and response to amphetamine in M1 muscarinic acetylcholine receptor-deficient mice. Proc Natl Acad Sci USA 2001; 98: 15312–15317, [PUBMED], [INFOTRIEVE], [CSA], [CROSSREF]
- Gomeza J, Zhang L, Kostenis E, Felder C, Bymaster F, Brodkin J, Shannon H, Xia B, Deng C, Wess J. Enhancement of D1 dopamine receptor-mediated locomotor stimulation in M(4) muscarinic acetylcholine receptor knockout mice. Proc Natl Acad Sci USA 1999b; 96: 10483–10488, [PUBMED], [INFOTRIEVE], [CSA]
- Yamada M, Lamping K G, Duttaroy A, Zhang W, Cui Y, Bymaster F P, McKinzie D L, Felder C C, Deng C X, Faraci F M, Wess J. Cholinergic dilation of cerebral blood vessels is abolished in M(5) muscarinic acetylcholine receptor knockout mice. Proc Natl Acad Sci USA 2001a; 98: 14096–14101, [PUBMED], [INFOTRIEVE], [CSA]
- Berkeley J L, Gomeza J, Wess J, Hamilton S E, Nathanson N M, Levey A I. M1 muscarinic acetylcholine receptors activate extracellular signal-regulated kinase in CA1 pyramidal neurons in mouse hippocampal slices. Mol Cell Neurosci 2001; 18: 512–524, [PUBMED], [INFOTRIEVE], [CSA], [CROSSREF]
- Stengel P W, Yamada M, Wess J, Cohen M L. M(3)-receptor knockout mice: Muscarinic receptor function in atria, stomach fundus, urinary bladder, and trachea. Am J Physiol Regul Integr Comp Physiol 2002; 282: R1443–R1449, [PUBMED], [INFOTRIEVE], [CSA]
- Yamada M, Miyakawa T, Duttaroy A, Yamanaka A, Moriguchi T, Makita R, Ogawa M, Chou C J, Xia B, Crawley J N, Felder C C, Deng C X, Wess J. Mice lacking the M3 muscarinic acetylcholine receptor are hypophagic and lean. Nature 2001b; 410: 207–212, [PUBMED], [INFOTRIEVE], [CSA], [CROSSREF]
- Cheng Y, Prusoff W H. Relationship between the inhibition constant (K1) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction. Biochem Pharmacol 1973; 22: 3099–3108, [PUBMED], [INFOTRIEVE], [CSA], [CROSSREF]
- Burstein E S, Spalding T A, Brann M R. Structure/function relationships of a G-protein coupling pocket formed by the third intracellular loop of the m5 muscarinic receptor. Biochemistry 1998a; 37: 4052–4058, [PUBMED], [INFOTRIEVE], [CSA], [CROSSREF]
- Zeng F Y, McLean A J, Milligan G, Lerner M, Chalmers D T, Behan D P. Ligand specific up-regulation of a Renilla reniformis luciferase-tagged, structurally unstable muscarinic M3 chimeric G protein-coupled receptor. Mol Pharmacol 2003; 64: 1474–1484, [PUBMED], [INFOTRIEVE], [CSA], [CROSSREF]
- Schmidt C, Li B, Bloodworth L, Erlenbach I, Zeng F Y, Wess J. Random mutagenesis of the M3 muscarinic acetylcholine receptor expressed in yeast. Identification of point mutations that “silence” a constitutively active mutant M3 receptor and greatly impair receptor/G protein coupling. J Biol Chem 2003; 278: 30248–30260, [PUBMED], [INFOTRIEVE], [CSA], [CROSSREF]