The conformational switch in 7-transmembrane receptors: the muscarinic receptor paradigm.

No abstract is available for this paper.

• Publication year

  1999

• Venue

  European Journal of Pharmacology

• Publication date

  1999-06-30

• Fields of study

  Biology, Medicine, Chemistry

• Identifiers
  DOI 10.1016/S0014-2999(99)00297-6PMID 10443581
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar, PubMed

• No claims are published for this paper.

• No concepts are published for this paper.

• G-protein-coupled receptors.

  2008cited by this paper
• Conformational Changes in Rhodopsin

  1999cited by this paper
• The Functional Topography of Transmembrane Domain 3 of the M1 Muscarinic Acetylcholine Receptor, Revealed by Scanning Mutagenesis*

  1999cited by this paper
• TYR381 in transmembrane domain six of the rat M1-muscarinic acetylcholine receptor plays a dual role in receptor function

  1999cited by this paper
• Folding funnels and frustration in off-lattice minimalist protein landscapes.

  1998cited by this paper
• A hydrophobic cluster between transmembrane helices 5 and 6 constrains the thyrotropin-releasing hormone receptor in an inactive conformation.

  1998cited by this paper
• Rhodopsin-family receptors associate with small G proteins to activate phospholipase D

  1998cited by this paper
• G Protein-coupled Receptors

  1998cited by this paper
• Analysis of zinc binding sites in protein crystal structures

  1998cited by this paper
• Identification of a Ligand-dependent Switch within a Muscarinic Receptor*

  1998cited by this paper
• Opioid receptor three-dimensional structures from distance geometry calculations with hydrogen bonding constraints.

  1998cited by this paper
• Structure/function relationships of a G-protein coupling pocket formed by the third intracellular loop of the m5 muscarinic receptor.

  1998cited by this paper
• Combined biophysical and biochemical information confirms arrangement of transmembrane helices visible from the three-dimensional map of frog rhodopsin.

  1998cited by this paper
• Constitutive activation of opsin by mutation of methionine 257 on transmembrane helix 6.

  1998cited by this paper
• Molecular basis of receptor/G-protein-coupling selectivity.

  1998cited by this paper
• Scanning mutagenesis of transmembrane domain 3 of the M1 muscarinic acetylcholine receptor.

  1998cited by this paper
• The Second Intracellular Loop of the m5 Muscarinic Receptor Is the Switch Which Enables G-protein Coupling*

  1998cited by this paper
• Certain activating mutations within helix 6 of the human luteinizing hormone receptor may be explained by alterations that allow transmembrane regions to activate Gs.

  1998cited by this paper
• Examination of ligand-induced conformational changes in the beta 2-adrenergic receptor by fluorescence spectroscopy.

  1998cited by this paper
• Agonist-independent regulation of constitutively active G-protein-coupled receptors.

  1998cited by this paper
• Characterisation of an improved two-dimensional p22121 crystal from bovine rhodopsin.

  1998cited by this paper
• Lipid patches in membrane protein oligomers: crystal structure of the bacteriorhodopsin-lipid complex.

  1998cited by this paper
• Light-induced exposure of the cytoplasmic end of transmembrane helix seven in rhodopsin.

  1998cited by this paper
• Neurobiology of the Caenorhabditis elegans genome.

  1998cited by this paper
• GPCRDB: an information system for G protein-coupled receptors

  1998cited by this paper
• G Protein-coupled Receptors

  1998cited by this paper
• Constitutive Activation of the β2 Adrenergic Receptor Alters the Orientation of Its Sixth Membrane-spanning Segment*

  1997cited by this paper
• Molecular basis of receptor/G protein coupling selectivity studied by coexpression of wild type and mutant m2 muscarinic receptors with mutant G alpha(q) subunits.

  1997cited by this paper
• Structural Instability of a Constitutively Active G Protein-coupled Receptor

  1997cited by this paper
• Interactions between Conserved Residues in Transmembrane Helices 1, 2, and 7 of the Thyrotropin-releasing Hormone Receptor*

  1997cited by this paper
• Arrangement of rhodopsin transmembrane α-helices

  1997cited by this paper
• How receptors talk to trimeric G proteins.

  1997cited by this paper
• Transducin-α C-terminal Peptide Binding Site Consists of C-D and E-F Loops of Rhodopsin*

  1997cited by this paper
• Constitutive activation of the m5 muscarinic receptor by a series of mutations at the extracellular end of transmembrane 6.

  1997cited by this paper
• Agonists induce conformational changes in transmembrane domains III and VI of the β2 adrenoceptor

  1997cited by this paper
• Receptor and betagamma binding sites in the alpha subunit of the retinal G protein transducin.

  1997cited by this paper
• Up-regulation of the levels of expression and function of a constitutively active mutant of the hamster alpha1B-adrenoceptor by ligands that act as inverse agonists.

  1997cited by this paper
• The activation process of the alpha1B-adrenergic receptor: potential role of protonation and hydrophobicity of a highly conserved aspartate.

  1997cited by this paper
• Structure and function in rhodopsin: rhodopsin mutants with a neutral amino acid at E134 have a partially activated conformation in the dark state.

  1997cited by this paper
• 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.

  1997cited by this paper
• The transmembrane 7-alpha-bundle of rhodopsin: distance geometry calculations with hydrogen bonding constraints.

  1997cited by this paper
• Cysteine scanning mutagenesis of transmembrane domain V of the M1 muscarinic receptor

  1997cited by this paper
• The steric trigger in rhodopsin activation.

  1997cited by this paper
• Structure and function in rhodopsin: packing of the helices in the transmembrane domain and folding to a tertiary structure in the intradiscal domain are coupled.

  1997cited by this paper
• Transducin-alpha C-terminal peptide binding site consists of C-D and E-F loops of rhodopsin.

  1997cited by this paper
• Receptor and βγ Binding Sites in the α Subunit of the Retinal G Protein Transducin

  1997cited by this paper
• The first and second cytoplasmic loops of the G-protein receptor, rhodopsin, independently form beta-turns.

  1997cited by this paper
• Arrangement of rhodopsin transmembrane alpha-helices.

  1997cited by this paper
• Crystal structure of a G-protein beta gamma dimer at 2.1A resolution.

  1996cited by this paper
• Structural features and light-dependent changes in the cytoplasmic interhelical E-F loop region of rhodopsin: a site-directed spin-labeling study.

  1996cited by this paper
• Molecular architecture of G protein‐coupled receptors

  1996cited by this paper
• Molecular aspects of muscarinic receptor assembly and function.

  1996cited by this paper
• Crystal structure of a G-protein βγ dimer at 2.1 Å resolution

  1996cited by this paper
• Activating mutations of rhodopsin and other G protein-coupled receptors.

  1996cited by this paper
• Requirement of Rigid-Body Motion of Transmembrane Helices for Light Activation of Rhodopsin

  1996cited by this paper
• Chapter 13 Molecular aspects of muscarinic receptor assembly and function

  1996cited by this paper
• Molecular biology of muscarinic acetylcholine receptors.

  1996cited by this paper
• Amino Acid Side Chains That Define Muscarinic Receptor/G-protein Coupling

  1996cited by this paper
• Structure of a G-protein-coupling Domain of a Muscarinic Receptor Predicted by Random Saturation Mutagenesis (*)

  1996cited by this paper
• Crystal structure of a GA protein βγdimer at 2.1 Å resolution

  1996cited by this paper
• Rhodopsin activation blocked by metal-ion-binding sites linking transmembrane helices C and F

  1996cited by this paper
• Constitutive activation of a single effector pathway: evidence for multiple activation states of a G protein-coupled receptor.

  1996cited by this paper
• Na+ ions binding to the bradykinin B2 receptor suppress agonist-independent receptor activation.

  1996cited by this paper
• The conserved seven-transmembrane sequence NP(X)2,3Y of the G-protein-coupled receptor superfamily regulates multiple properties of the beta 2-adrenergic receptor.

  1995cited by this paper
• Mapping light-dependent structural changes in the cytoplasmic loop connecting helices C and D in rhodopsin: a site-directed spin labeling study.

  1995cited by this paper
• Efficient Interaction with a Receptor Requires a Specific Type of Prenyl Group on the G Protein γ Subunit (*)

  1995cited by this paper
• In vivo assembly of rhodopsin from expressed polypeptide fragments.

  1995cited by this paper
• Mapping of Single Amino Acid Residues Required for Selective Activation of G by the m3 Muscarinic Acetylcholine Receptor (*)

  1995cited by this paper
• Identification of an intracellular tyrosine residue critical for muscarinic receptor-mediated stimulation of phosphatidylinositol hydrolysis.

  1994cited by this paper
• Acetylcholine mustard labels the binding site aspartate in muscarinic acetylcholine receptors.

  1994cited by this paper
• Structure and dynamics of the active site gorge of acetylcholinesterase: Synergistic use of molecular dynamics simulation and X‐ray crystallography

  1994cited by this paper
• Locating ligand-binding sites in 7TM receptors by protein engineering.

  1994cited by this paper
• Conserved tyrosines in the alpha subunit of the nicotinic acetylcholine receptor stabilize quaternary ammonium groups of agonists and curariform antagonists.

  1994cited by this paper
• Structure and function in rhodopsin: replacement by alanine of cysteine residues 110 and 187, components of a conserved disulfide bond in rhodopsin, affects the light-activated metarhodopsin II state.

  1994cited by this paper
• Molecular basis of muscarinic receptor function

  1993cited by this paper
• A common motif in G-protein-coupled seven transmembrane helix receptors

  1993cited by this paper
• A mutation-induced activated state of the beta 2-adrenergic receptor. Extending the ternary complex model.

  1993cited by this paper
• Hydrophobic amino acid in the i2 loop plays a key role in receptor-G protein coupling.

  1993cited by this paper
• Functional role of proline and tryptophan residues highly conserved among G protein‐coupled receptors studied by mutational analysis of the m3 muscarinic receptor.

  1993cited by this paper
• Molecular basis of muscarinic acetylcholine receptor function.

  1993cited by this paper
• The probable arrangement of the helices in G protein‐coupled receptors.

  1993cited by this paper
• Role of conserved threonine and tyrosine residues in acetylcholine binding and muscarinic receptor activation. A study with m3 muscarinic receptor point mutants.

  1992cited by this paper
• Mechanism of activation and inactivation of opsin: role of Glu113 and Lys296.

  1992cited by this paper
• Three-dimensional models of neurotransmitter G-binding protein-coupled receptors.

  1991cited by this paper
• Muscarinic acetylcholine receptors. Peptide sequencing identifies residues involved in antagonist binding and disulfide bond formation.

  1990cited by this paper
• Site-directed mutagenesis of m1 muscarinic acetylcholine receptors: conserved aspartic acids play important roles in receptor function.

  1989cited by this paper
• Cysteine residues 110 and 187 are essential for the formation of correct structure in bovine rhodopsin.

  1988cited by this paper
• The opsin family of proteins.

  1986cited by this paper
• BIOCHEMICAL STUDIES ON MUSCARINIC ACETYLCHOLINE RECEPTORS

  1976cited by this paper
• ON THE NATURE OF ALLOSTERIC TRANSITIONS: A PLAUSIBLE MODEL.

  1965cited by this paper

• Sartan-AT receptor interactions: evidence for insurmountable antagonism and inverse agonism

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• G Protein-Coupled Receptor Genetics

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• Using In Vitro Mutagenesis to Characterize Structure-Function Relationships in G Protein-Coupled Receptors

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• GPCR activation: a mutagenic spotlight on crystal structures.

  2013cites this paper
• Investigation of the activation mechanism and structural characterization of the CGRP receptor

  2013cites this paper
• The use of site-directed mutagenesis to study GPCRs.

  2011cites this paper
• Interaction of Transient Receptor Potential Vanilloid 1 (TRPV1) with G-protein coupled receptors and TRP ion channels

  2011cites this paper
• Signaling Diversity Mediated by Muscarinic Acetylcholine Receptor Subtypes and Evidence for Functional Selectivity

  2009cites this paper
• Sartan-AT1 receptor interactions: in vitro evidence for insurmountable antagonism and inverse agonism.

  2009cites this paper
• Homology modeling of MT1 and MT2 receptors.

  2008cites this paper
• Molekulare Mechanismen der Schmerzinhibition durch Opioide beim Entzündungsschmerz

  2008cites this paper
• Identification of a Novel Ligand Binding Residue Arg38(1.35) in the Human Gonadotropin-Releasing Hormone Receptor

  2008influential citation
• Human GnRH Receptor

  2007cites this paper
• Functional Analysis of Transmembrane Domain 2 of the M1 Muscarinic Acetylcholine Receptor*

  2007cites this paper
• Identification of a Novel Ligand Binding Residue Arg 38(1.35) in the Human GnRH Receptor

  2007influential citation
• Molecular basis of ligand binding to the M1 muscarinic acetylcholine receptor: Focus on the second extracellular loop.

  2006cites this paper
• A combined ligand-based and target-based drug design approach for G-protein coupled receptors: application to salvinorin A, a selective kappa opioid receptor agonist

  2006cites this paper
• Logic and Mechanism of an Evolutionarily Conserved Interaction in PDZ Domain

  2006cites this paper
• Neuronal control of skin function: the skin as a neuroimmunoendocrine organ.

  2006cites this paper
• Muscarinic acetylcholine receptors.

  2006cites this paper
• 19 CGRP: a Multifunctional Neuropeptide

  2006cites this paper
• Cannabinoid receptors as therapeutic targets.

  2006cites this paper
• G protein‐coupled receptors: a count of 1001 conformations

  2005cites this paper
• Cysteine 2.59(89) in the Second Transmembrane Domain of Human CB2 Receptor Is Accessible within the Ligand Binding Crevice: Evidence for Possible CB2 Deviation from a Rhodopsin Template

  2005cites this paper
• A key role for transmembrane prolines in calcitonin receptor-like receptor agonist binding and signalling: implications for family B G-protein-coupled receptors.

  2005cites this paper
• (-)-7′-Isothiocyanato-11-hydroxy-1′,1′-dimethylheptylhexahydrocannabinol (AM841), a High-Affinity Electrophilic Ligand, Interacts Covalently with a Cysteine in Helix Six and Activates the CB1 Cannabinoid Receptor

  2005cites this paper
• Different Environments for a Realistic Simulation of GPCRs‐Application to the M2 Muscarinic Receptor

  2005cites this paper
• Cannabinoid receptors and their ligands: ligand-ligand and ligand-receptor modeling approaches.

  2005cites this paper
• Mutations Remote from the Human Gonadotropin-releasing Hormone (GnRH) Receptor-binding Sites Specifically Increase Binding Affinity for GnRH II but Not GnRH I

  2005cites this paper
• Analysis of structure-activity relationships for MT2 selective antagonists by melatonin MT1 and MT2 receptor models.

  2005cites this paper
• Gonadotropin-releasing hormone receptors.

  2004cites this paper
• Toward the active conformations of rhodopsin and the β2‐adrenergic receptor

  2004cites this paper
• High-Throughput Modeling of Human G-Protein Coupled Receptors: Amino Acid Sequence Alignment, Three-Dimensional Model Building, and Receptor Library Screening

  2004cites this paper
• Structural Mimicry in Class A G Protein-coupled Receptor Rotamer Toggle Switches

  2004cites this paper
• 3-Indolyl-1-naphthylmethanes: new cannabimimetic indoles provide evidence for aromatic stacking interactions with the CB(1) cannabinoid receptor.

  2003cites this paper
• Regulatory Aspects of Neuroimmunology in the Skin

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• An aromatic microdomain at the cannabinoid CB(1) receptor constitutes an agonist/inverse agonist binding region.

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• Protein‐based virtual screening of chemical databases. II. Are homology models of g‐protein coupled receptors suitable targets?

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• Molecular Modelling Untersuchungen an der Bindungsstelle allosterischer Modulatoren des Muscarin M2 Rezeptors

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• Structural studies of metarhodopsin II, the activated form of the G-protein coupled receptor, rhodopsin.

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• Two mutations in extracellular loop 2 of the human GnRH receptor convert an antagonist to an agonist.

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