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

Identification of two related pentapeptides from the brain with potent opiate agonist activity

1975 • 3,780 citations

Identification of a major co-receptor for primary isolates of HIV-1

1996 • 3,649 citations

The GTPase superfamily: conserved structure and molecular mechanism

1991 • 3,365 citations

PHARMACOLOGY AND FUNCTIONS OF METABOTROPIC GLUTAMATE RECEPTORS

1997 • 3,070 citations

Molecular cloning of a functional thrombin receptor reveals a novel proteolytic mechanism of receptor activation

1991 • 2,981 citations

[19] Integrated methods for the construction of three-dimensional models and computational probing of structure-function relations in G protein-coupled receptors

1995 • 2,811 citations

RAMPs regulate the transport and ligand specificity of the calcitonin-receptor-like receptor

1998 • 2,076 citations

MODEL SYSTEMS FOR THE STUDY OF SEVEN-TRANSMEMBRANE-SEGMENT RECEPTORS

1991 • 1,357 citations

GABAB-receptor subtypes assemble into functional heteromeric complexes

1998 • 1,163 citations

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

1996 • 1,159 citations

Heterodimerization is required for the formation of a functional GABAB receptor

1998 • 1,156 citations

G-protein-coupled receptor heterodimerization modulates receptor function

1999 • 1,146 citations

The Many Faces of G Protein Signaling

1998 • 1,137 citations

The 2.0 Å crystal structure of a heterotrimeric G protein

1996 • 1,118 citations

THE ROLE OF RECEPTOR KINASES AND ARRESTINS IN G PROTEIN–COUPLED RECEPTOR REGULATION

1998 • 1,074 citations

GABAB receptors function as a heteromeric assembly of the subunits GABABR1 and GABABR2

1998 • 1,054 citations

Protease-activated receptor 3 is a second thrombin receptor in humans

1997 • 878 citations

Pigmentation phenotypes of variant extension locus alleles result from point mutations that alter MSH receptor function

1993 • 873 citations

Sequence Alignment of the G-Protein Coupled Receptor Superfamily

1992 • 847 citations

Projection structure of rhodopsin

1993 • 758 citations

The ligand-binding domain in metabotropic glutamate receptors is related to bacterial periplasmic binding proteins

1993 • 695 citations

Structure of a glutamate-receptor ligand-binding core in complex with kainate

1998 • 672 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

G‐protein‐coupled receptors: molecular mechanisms involved in receptor activation and selectivity of G‐protein recognition

1997 • 585 citations

Essential Role for G Protein-coupled Receptor Endocytosis in the Activation of Mitogen-activated Protein Kinase

1998 • 542 citations

Antagonists with negative intrinsic activity at delta opioid receptors coupled to GTP-binding proteins.

1989 • 519 citations

GCRDb: a G-protein-coupled receptor database.

1994 • 517 citations

Constitutively active mutants of rhodopsin

1992 • 513 citations

Metabotropic Glutamate Receptor 5 Is a Disulfide-linked Dimer

1996 • 512 citations

The two-state model of receptor activation

1995 • 492 citations

Rapid Identification of Subtype-Selective Agonists of the Somatostatin Receptor Through Combinatorial Chemistry

1998 • 455 citations

Arrangement of rhodopsin transmembrane α-helices

1997 • 449 citations

Molecular Basis of Receptor/G-Protein-Coupling Selectivity

1998 • 444 citations

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

1992 • 415 citations

Dimerization of the Extracellular Calcium-sensing Receptor (CaR) on the Cell Surface of CaR-transfected HEK293 Cells

1998 • 396 citations

THE LUTEINIZING HORMONE RECEPTOR

1998 • 393 citations

Rhodopsin activation blocked by metal-ion-binding sites linking transmembrane helices C and F

1996 • 389 citations

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

1996 • 377 citations

CP-154,526: a potent and selective nonpeptide antagonist of corticotropin releasing factor receptors.

1996 • 375 citations

Rhodopsin mutation G90D and a molecular mechanism for congenital night blindness

1994 • 373 citations

The family of G‐protein‐coupled receptors

1995 • 369 citations

Three-dimensional models of neurotransmitter G-binding protein-coupled receptors.

1991 • 330 citations

Coexpression studies with mutant muscarinic/adrenergic receptors provide evidence for intermolecular "cross-talk" between G-protein-linked receptors.

1993 • 321 citations

Locating ligand-binding sites in 7tm receptors by protein engineering

1994 • 282 citations

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

1995 • 278 citations

Dopamine D2 Receptor Dimers and Receptor-Blocking Peptides

1996 • 266 citations

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

1994 • 260 citations

The chemokine monocyte chemoattractant protein-1 induces functional responses through dimerization of its receptor CCR2

1999 • 229 citations

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

1996 • 226 citations

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

1994 • 226 citations

The Extracellular Calcium-Sensing Receptor: Its Role in Health and Disease

1998 • 218 citations

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

1993 • 218 citations

Secretin and vasoactive intestinal peptide receptors: Members of a unique family of G protein–coupled receptors

1998 • 217 citations

Different binding epitopes on the NK1 receptor for substance P and a non-peptide antagonist

1993 • 213 citations

Rhodopsin-family receptors associate with small G proteins to activate phospholipase D

1998 • 211 citations

Specificity of the thrombin receptor for agonist peptide is defined by its extracellular surface

1994 • 210 citations

Identification of a receptor/G-protein contact site critical for signaling specificity and G-protein activation.

1995 • 204 citations

G-protein diseases furnish a model for the turn-on switch

1998 • 192 citations

Amino–aromatic interaction between histidine 197 of the neurokinin-1 receptor and CP 96345

1993 • 185 citations

Disulfide Bonds in the Extracellular Calcium-Polyvalent Cation-sensing Receptor Correlate with Dimer Formation and Its Response to Divalent Cations in Vitro

1998 • 185 citations

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

1991 • 185 citations

Parathyroid Hormone-Receptor Interactions Identified Directly by Photocross-linking and Molecular Modeling Studies

1998 • 184 citations

Thyrotropin-luteinizing hormone/chorionic gonadotropin receptor extracellular domain chimeras as probes for thyrotropin receptor function.

1991 • 183 citations

Expression of Dopamine D3 Receptor Dimers and Tetramers in Brain and in Transfected Cells

1997 • 168 citations

Conversion of antagonist-binding site to metal-ion site in the tachykinin NK-1 receptor

1995 • 167 citations

Mutation of Asp74 of the rat angiotensin II receptor confers changes in antagonist affinities and abolishes G-protein coupling.

1993 • 162 citations

Mapping the binding-site crevice of the dopamine D2 receptor by the substituted-cysteine accessibility method

1995 • 162 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

Mutation of Asn111 in the Third Transmembrane Domain of the AT1A Angiotensin II Receptor Induces Its Constitutive Activation

1997 • 155 citations

Binding domains of stimulatory and inhibitory thyrotropin (TSH) receptor autoantibodies determined with chimeric TSH-lutropin/chorionic gonadotropin receptors.

1991 • 155 citations

Constitutive Activation of Opsin by Mutation of Methionine 257 on Transmembrane Helix 6

1998 • 141 citations

Role of the large extracellular domain of metabotropic glutamate receptors in agonist selectivity determination.

1993 • 141 citations

Photoactivated Conformational Changes in Rhodopsin: A Time-Resolved Spin Label Study

1993 • 140 citations

Constitutive activation of the TSH receptor by spontaneous mutations affecting the N‐terminal extracellular domain

1997 • 138 citations

Probing the Structure and Function of the Tachykinin Neurokinin-2 Receptor through Biosynthetic Incorporation of Fluorescent Amino Acids at Specific Sites

1996 • 133 citations

The Second Intracellular Loop of the m5 Muscarinic Receptor Is the Switch Which Enables G-protein Coupling

1998 • 125 citations

Transmembrane Regions V and VI of the Human Luteinizing Hormone Receptor Are Required for Constitutive Activation by a Mutation in the Third Intracellular Loop

1996 • 122 citations

A Transmembrane Domain-derived Peptide Inhibits D1 Dopamine Receptor Function without Affecting Receptor Oligomerization

1998 • 120 citations

Molecular basis for the species selectivity of the substance P antagonist CP-96,345.

1993 • 118 citations

Differentiation between binding sites for angiotensin II and nonpeptide antagonists on the angiotensin II type 1 receptors.

1994 • 117 citations

Similarities and Differences in RANTES- and (AOP)-RANTES–triggered Signals: Implications for Chemotaxis

1999 • 117 citations

Dimerization of the Calcium-sensing Receptor Occurs within the Extracellular Domain and Is Eliminated by Cys → Ser Mutations at Cys101 and Cys236

1999 • 115 citations

Residues in the Seventh Membrane-Spanning Segment of the Dopamine D2 Receptor Accessible in the Binding-Site Crevice

1996 • 109 citations

Evidence for a Ligand Interaction Site at the Amino-Terminus of the Parathyroid Hormone (PTH)/PTH-related Protein Receptor from Cross-linking and Mutational Studies

1998 • 109 citations

A model for the structure of bacteriorhodopsin based on high resolution electron cryomicroscopy

1990 • 108 citations

Modeling of transmembrane seven helix bundles

1993 • 106 citations

A General Method for Mapping Tertiary Contacts between Amino Acid Residues in Membrane-Embedded Proteins

1995 • 103 citations

Residues in the Fifth Membrane-Spanning Segment of the Dopamine D2 Receptor Exposed in the Binding-Site Crevice

1995 • 102 citations

Multiple Extracellular Loop Domains Contribute Critical Determinants for Agonist Binding and Activation of the Secretin Receptor

1996 • 97 citations

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

1998 • 95 citations

Highly Conserved Aspartate 68, Tryptophane 73 and Glycine 109 in the N-Terminal Extracellular Domain of the Human VIP Receptor Are Essential for Its Ability to Bind VIP

1995 • 94 citations

Extracellular Domains of the Bradykinin B2 Receptor Involved in Ligand Binding and Agonist Sensing Defined by Anti-peptide Antibodies

1996 • 93 citations

Fourier Transform Infrared Difference Spectra of Intermediates in Rhodopsin Bleaching

1983 • 92 citations

Residues in the Membrane-spanning and Extracellular Loop Regions of the Parathyroid Hormone (PTH)-2 Receptor Determine Signaling Selectivity for PTH and PTH-related Peptide

1997 • 91 citations

Neuropeptide Y and the nonpeptide antagonist BIBP 3226 share an overlapping binding site at the human Y1 receptor.

1996 • 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

Identification of a Ligand-dependent Switch within a Muscarinic Receptor

1998 • 88 citations

Conformational Changes in Rhodopsin Probed by Surface Plasmon Resonance Spectroscopy

1994 • 87 citations

Connectivity and orientation of the seven helical bundle in the tachykinin NK-1 receptor probed by zinc site engineering.

1996 • 86 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

Molecular Mechanism of Action of Non-peptide Ligands for Peptide Receptors

1995 • 78 citations

Fourier transform infrared difference spectroscopy of rhodopsin mutants: Light activation of rhodopsin causes hydrogen-bonding change in residue aspartic acid-83 during meta II formation

1993 • 74 citations

A model of the lutropin/choriogonadotropin receptor: insights into the structural and functional effects of constitutively activating mutations

1997 • 72 citations

Mutational Analysis of the Relative Orientation of Transmembrane Helices I and VII in G Protein-coupled Receptors

1995 • 71 citations

Monoclonal antibodies to purified muscarinic receptor display agonist-like activity.

1984 • 70 citations

Identification of an intracellular tyrosine residue critical for muscarinic receptor-mediated stimulation of phosphatidylinositol hydrolysis.

1994 • 70 citations

Two nonpeptide tachykinin antagonists act through epitopes on corresponding segments of the NK1 and NK2 receptors.

1993 • 69 citations

Structure of a G-protein-coupling Domain of a Muscarinic Receptor Predicted by Random Saturation Mutagenesis

1996 • 66 citations

Projection Structure of an Invertebrate Rhodopsin

1996 • 64 citations

A Segment of Five Amino Acids in the Second Extracellular Loop of the Cholecystokinin-B Receptor Is Essential for Selectivity of the Peptide Agonist Gastrin

1996 • 63 citations

Structure and Function of G Protein-Coupled Receptors

1994 • 63 citations

Constitutive Activation of the Human Vasoactive Intestinal Peptide 1 Receptor, a Member of the New Class II Family of G Protein-coupled Receptors

1998 • 62 citations

Characterization of Non-peptide Antagonist and Peptide Agonist Binding Sites of the NK1 Receptor with Fluorescent Ligands

1997 • 62 citations

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

1999 • 61 citations

The role of histidine 265 in antagonist binding to the neurokinin-1 receptor.

1994 • 61 citations

Genetic transfer of a nonpeptide antagonist binding site to a previously unresponsive angiotensin receptor.

1995 • 57 citations

Leutropin/beta-adrenergic receptor chimeras bind choriogonadotropin and adrenergic ligands but are not expressed at the cell surface

1991 • 57 citations

Antibodies against specific extracellular epitopes of the glucagon receptor block glucagon binding.

1996 • 53 citations

Functional role of a cytoplasmic aromatic amino acid in muscarinic receptor-mediated activation of phospholipase C

1994 • 49 citations

Interaction of glutamine 165 in the fourth transmembrane segment of the human neurokinin-1 receptor with quinuclidine antagonists.

1994 • 49 citations

Five Out of Six Tryptophan Residues in the N -Terminal Extracellular Domain of the Rat GLP-1 Receptor Are Essential for its Ability to Bind GLP-1

1997 • 48 citations

The species selectivity of chemically distinct tachykinin nonpeptide antagonists is dependent on common divergent residues of the rat and human neurokinin-1 receptors.

1994 • 48 citations

Vasoactive Intestinal Polypeptide and Pituitary Adenylate Cyclase-Activating Polypeptide Receptor Chimeras Reveal Domains That Determine Specificity of Vasoactive Intestinal Polypeptide Binding and Activation

1997 • 46 citations

Aspartate 196 in the First Extracellular Loop of the Human VIP1 Receptor Is Essential for VIP Binding and VIP-Stimulated cAMP Production

1997 • 44 citations

Somatic Mutations in the Thyrotropin Receptor Gene Cause Hyperfunctioning Thyroid Adenomas

1994 • 43 citations

Identification of a Polar Region in Transmembrane Domain 6 That Regulates the Function of the G Protein-Coupled α-Factor Receptor

1998 • 43 citations

Separable Binding Sites for the Natural Agonist Endothelin-1 and the Non-Peptide Antagonist Bosentan on Human Endothelin-A Receptors

1995 • 42 citations

Mutations within the Cholecystokinin-B/Gastrin Receptor Ligand ‘Pocket’ Interconvert the Functions of Nonpeptide Agonists and Antagonists

1998 • 33 citations

Localization of Agonist- and Antagonist-Binding Domains of Human Corticotropin-Releasing Factor Receptors

1997 • 31 citations

The agonist selectivity of a class III metabotropic glutamate receptor, human mGluR4a, is determined by the N-terminal extracellular domain

1995 • 28 citations

A Mutation Changes Ligand Selectivity and Transmembrane Signaling Preference of the Neurokinin-1 Receptor

1997 • 27 citations

Evidence for a common molecular mode of action for chemically distinct nonpeptide antagonists at the neurokinin-1 (substance P) receptor.

1994 • 26 citations

Intramolecular interactions in muscarinic acetylcholine receptors studied with chimeric m2/m5 receptors.

1994 • 25 citations

Modeling of G-Protein Coupled Receptors with Bacteriorhodopsin as a Template. A Novel Approach Based on Interaction Energy Differences

1994 • 22 citations

Derivation of Functional Antagonists Using N-Terminal Extracellular Domain of Gonadotropin and Thyrotropin Receptors

1997 • 20 citations

Adrenergic Receptors As Models For G Protein-Coupled Receptors

1992 • 18 citations

Multiple Regions of Ligand Discrimination Revealed by Analysis of Chimeric Parathyroid Hormone 2 (PTH2) and PTH/PTH-Related Peptide (PTHrP) Receptors

1998 • 17 citations

Arginine 186 in the Extracellular N-Terminal Region of the Human Parathyroid Hormone 1 Receptor Is Essential for Contact with Position 13 of the Hormone

1998 • 16 citations

Constitutive Activity of Glucagon Receptor Mutants

1997 • 16 citations

Mutational analyses of the extracellular domain of the full-length lutropin/choriogonadotropin receptor suggest leucine-rich repeats 1-6 are involved in hormone binding

1996 • 16 citations

Determinants for calcitonin analog interaction with the calcitonin receptor N-terminus and transmembrane-loop regions

1996 • 15 citations

Tachykinin non-peptide antagonists: binding domain and molecular mode of action

1995 • 15 citations

Fourier transform infrared spectroscopy indicates a major conformational rearrangement in the activation of rhodopsin

1995 • 14 citations

A single amino acid of the cholecystokinin-B/gastrin receptor determines specificity for non-peptide antagonists

1993 • 5 citations

Structure/function of muscarinic receptor coupling to G proteins: random-saturation mutagenesis identifies a critical determinant of receptor affinity for G proteins

1995 • 4 citations