G Protein-Coupled Receptor Structural Motifs: Relevance to the Opioid Receptors

Crystal Structure of Rhodopsin: A G Protein-Coupled Receptor

2000 • 5,539 citations

A mutation-induced activated state of the beta 2-adrenergic receptor. Extending the ternary complex model.

1993 • 1,213 citations

Uncovering Molecular Mechanisms Involved in Activation of G Protein-Coupled Receptors

2000 • 1,199 citations

Requirement of Rigid-Body Motion of Transmembrane Helices for Light Activation of Rhodopsin

1996 • 1,159 citations

Projection structure of rhodopsin

1993 • 758 citations

Activation of the β2-Adrenergic Receptor Involves Disruption of an Ionic Lock between the Cytoplasmic Ends of Transmembrane Segments 3 and 6

2001 • 605 citations

Palmitoylation of the human β2-adrenergic receptor

1989 • 599 citations

Advances in Determination of a High-Resolution Three-Dimensional Structure of Rhodopsin, a Model of G-Protein-Coupled Receptors (GPCRs)^,

2001 • 598 citations

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.

1992 • 587 citations

Conserved aspartic acid residues 79 and 113 of the beta-adrenergic receptor have different roles in receptor function.

1988 • 533 citations

In vitro mutagenesis and the search for structure-function relationships among G protein-coupled receptors

1992 • 470 citations

Heterodimerization of mu and delta opioid receptors: A role in opiate synergy.

2000 • 465 citations

Arrangement of rhodopsin transmembrane α-helices

1997 • 449 citations

Molecular Basis of Receptor/G-Protein-Coupling Selectivity

1998 • 444 citations

Structural Mimicry in G Protein-Coupled Receptors: Implications of the High-Resolution Structure of Rhodopsin for Structure-Function Analysis of Rhodopsin-Like Receptors

2001 • 442 citations

Modeling of G-protein-coupled receptors: application to dopamine, adrenaline, serotonin, acetylcholine, and mammalian opsin receptors

1992 • 415 citations

Two adjacent cysteine residues in the C‐terminal cytoplasmic fragment of bovine rhodopsin are palmitylated

1988 • 409 citations

β2 Adrenergic Receptor Activation

2002 • 405 citations

Constitutively active mutants of the alpha 1B-adrenergic receptor: role of highly conserved polar amino acids in receptor activation.

1996 • 377 citations

A highly conserved tyrosine residue in G protein-coupled receptors is required for agonist-mediated beta 2-adrenergic receptor sequestration.

1994 • 361 citations

Hypothesis about the function of membrane-buried proline residues in transport proteins.

1986 • 334 citations

G-protein-coupled receptor dimerization: modulation of receptor function

2001 • 307 citations

Regions of the alpha 1-adrenergic receptor involved in coupling to phosphatidylinositol hydrolysis and enhanced sensitivity of biological function.

1990 • 302 citations

Hinges, swivels and switches: the role of prolines in signalling via transmembrane α-helices

2000 • 286 citations

Low resolution structure of bovine rhodopsin determined by electron cryo-microscopy

1995 • 278 citations

A reciprocal mutation supports helix 2 and helix 7 proximity in the gonadotropin-releasing hormone receptor.

1994 • 260 citations

Site-directed mutagenesis of m1 muscarinic acetylcholine receptors: conserved aspartic acids play important roles in receptor function.

1989 • 258 citations

Role of palmitoylation/depalmitoylation reactions in G-protein-coupled receptor function

2002 • 255 citations

-mu opiate receptor. Charged transmembrane domain amino acids are critical for agonist recognition and intrinsic activity.

1994 • 236 citations

Constitutive arrestin-mediated desensitization of a human vasopressin receptor mutant associated with nephrogenic diabetes insipidus

2000 • 235 citations

Constitutively active mutants of the alpha 2-adrenergic receptor

1993 • 234 citations

A conserved carboxylic acid group mediates light-dependent proton uptake and signaling by rhodopsin.

1994 • 226 citations

Specific Tryptophan UV-Absorbance Changes Are Probes of the Transition of Rhodopsin to Its Active State

1996 • 226 citations

Internal Lysine Palmitoylation in Adenylate Cyclase Toxin from Bordetella pertussis

1994 • 223 citations

Site-directed mutagenesis of alpha 2A-adrenergic receptors: identification of amino acids involved in ligand binding and receptor activation by agonists.

1991 • 221 citations

Constitutive activation of opsin: Influence of charge at position 134 and size at position 296

1993 • 218 citations

Related Contribution of Specific Helix 2 and 7 Residues to Conformational Activation of the Serotonin 5-HT2A Receptor

1995 • 217 citations

Incomplete cross tolerance and multiple mu opioid peptide receptors

2001 • 208 citations

Mutation of a Highly Conserved Aspartic Acid in the β₂Adrenergic Receptor: Constitutive Activation, Structural Instability, and Conformational Rearrangement of Transmembrane Segment 6

1999 • 203 citations

Acylation of bovine rhodopsin by [3H]palmitic acid.

1984 • 200 citations

The activation process of the α _1B -adrenergic receptor: Potential role of protonation and hydrophobicity of a highly conserved aspartate

1997 • 196 citations

Similar Structures and Shared Switch Mechanisms of the β2-Adrenoceptor and the Parathyroid Hormone Receptor

1999 • 186 citations

Pivotal role for aspartate-80 in the regulation of dopamine D2 receptor affinity for drugs and inhibition of adenylyl cyclase.

1991 • 185 citations

The effect of mutations in the DRY motif on the constitutive activity and structural instability of the histamine H(2) receptor.

2000 • 184 citations

Opioid Receptor Three-Dimensional Structures from Distance Geometry Calculations with Hydrogen Bonding Constraints

1998 • 174 citations

Three-dimensional representations of G protein-coupled receptor structures and mechanisms

2002 • 173 citations

A Point Mutation of the α ₂ -Adrenoceptor that Blocks Coupling to Potassium but not Calcium Currents

1992 • 160 citations

A Cluster of Aromatic Residues in the Sixth Membrane-Spanning Segment of the Dopamine D2 Receptor Is Accessible in the Binding-Site Crevice

1998 • 159 citations

Site-directed mutagenesis and continuous expression of human beta-adrenergic receptors. Identification of a conserved aspartate residue involved in agonist binding and receptor activation.

1988 • 158 citations

Seven-transmembrane receptors: crystals clarify

2002 • 158 citations

Altered phosphorylation and desensitization patterns of a human beta 2-adrenergic receptor lacking the palmitoylated Cys341.

1993 • 158 citations

A single residue, aspartic acid 95, in the delta opioid receptor specifies selective high affinity agonist binding.

1993 • 146 citations

Characterization of mutant rhodopsins responsible for autosomal dominant retinitis pigmentosa. Mutations on the cytoplasmic surface affect transducin activation

1993 • 142 citations

Calmodulin Binding to G Protein-coupling Domain of Opioid Receptors

1999 • 128 citations

μ-Opioid Receptor-mediated ERK Activation Involves Calmodulin-dependent Epidermal Growth Factor Receptor Transactivation

2001 • 123 citations

Key Residues Defining the μ‐Opioid Receptor Binding Pocket: A Site‐Directed Mutagenesis Study

1997 • 120 citations

Conserved Helix 7 Tyrosine Acts as a Multistate Conformational Switch in the 5HT2C Receptor

2002 • 119 citations

Palmitoylated Cysteine 341 Modulates Phosphorylation of the β2-Adrenergic Receptor by the cAMP-dependent Protein Kinase

1996 • 116 citations

Mutational analysis of the highly conserved arginine within the Glu/Asp-Arg-Tyr motif of the alpha(1b)-adrenergic receptor: effects on receptor isomerization and activation.

2000 • 112 citations

Mutations of the Conserved DRS Motif in the Second Intracellular Loop of the Gonadotropin-Releasing Hormone Receptor Affect Expression, Activation, and Internalization

1997 • 110 citations

The Role of a Conserved Proline Residue in Mediating Conformational Changes Associated with Voltage Gating of Cx32 Gap Junctions

1999 • 104 citations

Cloning of the mouse 5-HT6 serotonin receptor and mutagenesis studies of the third cytoplasmic loop

2001 • 103 citations

Involvement of the Carboxyl Terminus of the Third Intracellular Loop of the Cannabinoid CB1 Receptor in Constitutive Activation of G_s

1999 • 98 citations

Characterisation of an improved two-dimensional p22121 crystal from bovine rhodopsin

1998 • 95 citations

Activating and Inactivating Mutations in N- and C-terminal i3 Loop Junctions of Muscarinic Acetylcholine Hm1 Receptors

1995 • 94 citations

Creation of a constitutively activated state of the 5-hydroxytryptamine2A receptor by site-directed mutagenesis: inverse agonist activity of antipsychotic drugs.

1998 • 93 citations

Molecular Docking Reveals a Novel Binding Site Model for Fentanyl at the μ-Opioid Receptor

2000 • 90 citations

Structure and function in rhodopsin: Rhodopsin mutants with a neutral amino acid at E134 have a partially activated conformation in the dark state

1997 • 89 citations

The D136A mutation of the V₂vasopressin receptor induces a constitutive activity which permits discrimination between antagonists with partial agonist and inverse agonist activities

1998 • 85 citations

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

1997 • 85 citations

Functional Role of a Conserved Motif in TM6 of the Rat μ Opioid Receptor: Constitutively Active and Inactive Receptors Result from Substitutions of Thr6.34(279) with Lys and Asp

2001 • 84 citations

Identification of Potential Tyrosine-containing Endocytic Motifs in the Carboxyl-tail and Seventh Transmembrane Domain of the Neurokinin 1 Receptor

1997 • 81 citations

Structure-Function of Muscarinic Receptor Coupling to G Proteins

1995 • 80 citations

Structural models for dimerization of G‐protein coupled receptors: The opioid receptor homodimers

2002 • 80 citations

Apparent Loss-of-Function Mutant GPCRs Revealed as Constitutively Desensitized Receptors

2002 • 79 citations

A Proposed Structure for Transmembrane Segment 7 of G Protein-Coupled Receptors Incorporating an Asn-Pro/Asp-Pro Motif

1998 • 73 citations

The conserved NPXnY motif present in the gastrin-releasing peptide receptor is not a general sequestration sequence.

1994 • 73 citations

Palmitoylation of the Vasopressin V1a Receptor Reveals Different Conformational Requirements for Signaling, Agonist-induced Receptor Phosphorylation, and Sequestration

2001 • 72 citations

Comparative modeling and molecular dynamics studies of the delta, kappa and mu opioid receptors

1997 • 67 citations

Charged amino acids required for signal transduction by the m3 muscarinic acetylcholine receptor.

1993 • 67 citations

Constitutive Activation of the μ Opioid Receptor by Mutation of D3.49(164), but Not D3.32(147): D3.49(164) Is Critical for Stabilization of the Inactive Form of the Receptor and for Its Expression

2001 • 65 citations

Structural and Functional Requirements for Agonist-induced Internalization of the Human Platelet-activating Factor Receptor

1997 • 64 citations

Critical Role of a Conserved Intramembrane Tyrosine Residue in Angiotensin II Receptor Activation

1995 • 64 citations

Mutation of a conserved serine in TM4 of opioid receptors confers full agonistic properties to classical antagonists.

1996 • 62 citations

Use of a Disulfide Cross-linking Strategy to Study Muscarinic Receptor Structure and Mechanisms of Activation

1999 • 61 citations

Naloxone Activation of μ-Opioid Receptors Mutated at a Histidine Residue Lining the Opioid Binding Cavity

1997 • 59 citations

Activating Mutations of the Serotonin 5‐HT_2C Receptor

1997 • 58 citations

Mutagenesis and peptide analysis of the DRY motif in the α2A adrenergic receptor: evidence for alternate mechanisms in G protein-coupled receptors

2002 • 54 citations

Dependence of agonist activation on an aromatic moiety in the DPLIY motif of the gonadotropin-releasing hormone receptor.

1996 • 48 citations

Inverse Agonist Up-Regulates the Constitutively Active D3.49(164)Q Mutant of the Rat μ-Opioid Receptor by Stabilizing the Structure and Blocking Constitutive Internalization and Down-Regulation

2001 • 47 citations

3D modeling, ligand binding and activation studies of the cloned mouse δ, μ and κ opioid receptors

1999 • 46 citations

Mutations of Tyr326 in the β2-adrenoceptor disrupt multiple receptor functions

1996 • 46 citations

Constitutively active mutants of the β1‐adrenergic receptor

1999 • 46 citations

Enhanced Stimulatory Adenylyl Cyclase Signaling during Opioid Dependence Is Associated with a Reduction in Palmitoylated G_sα

1997 • 46 citations

Replacement of Gln²⁸⁰ by His in TM6 of the human ORL1 receptor increases affinity but reduces intrinsic activity of opioids

1996 • 44 citations

Functional role of the spatial proximity of Asp114(2.50) in TMH 2 and Asn332(7.49) in TMH 7 of the μ opioid receptor

1999 • 43 citations

Alanine scanning mutagenesis of conserved arginine/lysine-arginine/lysine-X-X-arginine/lysine G protein-activating motifs on m1 muscarinic acetylcholine receptors.

1996 • 42 citations

Mutation of a highly conserved acidic residue present in the second intracellular loop of G-protein-coupled receptors does not impair hormone binding or signal transduction of the luteinizing hormone/chorionic gonadotropin receptor.

1993 • 42 citations

A Network of Conserved Intramolecular Contacts Defines the Off-state of the Transmembrane Switch Mechanism in a Seven-transmembrane Receptor

2000 • 42 citations

Analysis of the C-Terminal Tail of the Rat Thyrotropin-Releasing Hormone Receptor-1 in Interactions and Cointernalization with β-Arrestin 1-Green Fluorescent Protein

2001 • 41 citations

Effects of D3.49A, R3.50A, and A6.34E mutations on ligand binding and activation of the cannabinoid-2 (CB2) receptor

2003 • 40 citations

Calmodulin Regulation of Basal and Agonist‐Stimulated G Protein Coupling by the μ‐Opioid Receptor (OP₃) in Morphine‐Pretreated Cell

2000 • 40 citations

Activation of constitutive 5-hydroxytryptamine1B receptor by a series of mutations in the BBXXB motif: positioning of the third intracellular loop distal junction and its Goα protein interactions

1999 • 39 citations

Structure/Function Relationships of a G-Protein Coupling Pocket Formed by the Third Intracellular Loop of the m5 Muscarinic Receptor

1998 • 39 citations

A Mutation in the Hamster α_1B-Adrenergic Receptor that Differentiates Two Steps in the Pathway of Receptor Internalization

1997 • 35 citations

Mutagenesis of a Single Amino Acid in the Rat μ‐Opioid Receptor Discriminates Ligand Binding

1998 • 32 citations

The Local Environment at the Cytoplasmic End of TM6 of the μ Opioid Receptor Differs from Those of Rhodopsin and Monoamine Receptors: Introduction of an Ionic Lock between the Cytoplasmic Ends of Helices 3 and 6 by a L6.30(275)E Mutation Inactivates the μ Opioid Receptor and Reduces the Constitutive Activity of Its T6.34(279)K Mutant

2002 • 32 citations

Role of palmitoylation of conserved cysteine residues of luteinizing hormone/human choriogonadotropin receptors in receptor down-regulation1Supported by NIH grant HD 06656.1

1997 • 30 citations

Ligand-Selective Activation of μ-Opioid Receptor: Demonstrated with Deletion and Single Amino Acid Mutations of Third Intracellular Loop Domain

2003 • 29 citations

Basic Amino Acids at the C‐Terminus of the Third Intracellular Loop Are Required for the Activation of Phospholipase C by Cholecystokinin‐B Receptors

1997 • 28 citations

Palmitoylation of the rat μ opioid receptor

1998 • 28 citations

CONFORMATIONAL CHANGES OF CYTOSOLIC LOOPS OF BOVINE RHODOPSIN DURING THE TRANSITION TO METARHODOPSIN-II: AN INVESTIGATION BY FOURIER TRANSFORM INFRARED DIFFERENCE SPECTROSCOPY

1992 • 25 citations

A Conserved Arginine in the Distal Third Intracellular Loop of the μ‐Opioid Receptor Is Required for G Protein Activation

1999 • 25 citations

Chronic morphine treatment increases stimulatory beta-2 adrenoceptor signaling in A431 cells stably expressing the mu opioid receptor.

1997 • 22 citations

Switching Agonist/Antagonist Properties of Opiate Alkaloids at the δ Opioid Receptor Using Mutations Based on the Structure of the Orphanin FQ Receptor

2000 • 18 citations

Homology Models of μ-Opioid Receptor with Organic and Inorganic Cations at Conserved Aspartates in the Second and Third Transmembrane Domains

2000 • 18 citations

Mutagenesis of the mouse delta opioid receptor converts (-)-buprenorphine from a partial agonist to an antagonist.

1998 • 17 citations

Differential signalling of both wild-type and Thr 343 Arg dopamine D 2short receptor by partial agonists in a G-protein-dependent manner 1 1Abbreviations: NPA, propylnorapomorphine; PTX, Bordetella pertussis toxin; 7-OH-DPAT, 7-(hydroxy-2-(di-n-propylamino)tetralin; and (+)-UH 232, cis-(+)-5-methoxy-1-methyl-2-(di-n-propylamino)tetralin.

2001 • 13 citations

4 Molecular Modeling of Opioid Receptor-Ligand Complexes

2002 • 11 citations