Constitutive activity of G-protein-coupled receptors: cause of disease and common property of wild-type receptors

G PROTEINS: TRANSDUCERS OF RECEPTOR-GENERATED SIGNALS

1987 • 6,374 citations

Molecular tinkering of G protein-coupled receptors: an evolutionary success

1999 • 1,479 citations

G Protein-coupled Receptors

1998 • 1,292 citations

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

2000 • 1,199 citations

Glucose intolerance but normal satiety in mice with a null mutation in the glucagon–like peptide 1 receptor gene

1996 • 771 citations

A constitutively activating mutation of the luteinizing hormone receptor in familial male precocious puberty

1993 • 747 citations

Cloning and Functional Expression of the Human Islet GLP-1 Receptor: Demonstration That Exendin-4 Is an Agonist and Exendin-(9–39) an Antagonist of the Receptor

1993 • 533 citations

The two-state model of receptor activation

1995 • 492 citations

Inverse, protean, and ligand‐selective agonism: matters of receptor conformation

2001 • 403 citations

Agonist-independent activation of metabotropic glutamate receptors by the intracellular protein Homer

2001 • 397 citations

Germline mutations in the thyrotropin receptor gene cause non–autoimmune autosomal dominant hyperthyroidism

1994 • 376 citations

AgRP(83–132) Acts as an Inverse Agonist on the Human-Melanocortin-4 Receptor

2001 • 375 citations

Rhodopsin mutation G90D and a molecular mechanism for congenital night blindness

1994 • 373 citations

Inverse agonist activity of beta-adrenergic antagonists.

1994 • 357 citations

RNA Editing of the Human Serotonin 5-Hydroxytryptamine 2C Receptor Silences Constitutive Activity

1999 • 353 citations

Heterozygous missense mutation in the rhodopsin gene as a cause of congenital stationary night blindness

1993 • 323 citations

Cloning and characterization of a novel human histamine receptor.

2001 • 277 citations

Leydig-Cell Tumors Caused by an Activating Mutation of the Gene Encoding the Luteinizing Hormone Receptor

1999 • 274 citations

High agonist-independent activity is a distinguishing feature of the dopamine D1B receptor subtype.

1994 • 261 citations

Agouti-related protein functions as an inverse agonist at a constitutively active brain melanocortin-4 receptor

2001 • 248 citations

Inverse agonism of histamine H2 antagonist accounts for upregulation of spontaneously active histamine H2 receptors.

1996 • 235 citations

Structural and functional aspects of G protein-coupled receptor oligomerization

1998 • 213 citations

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

1998 • 192 citations

In vitro and in vivo pharmacological characterization of JTE-907, a novel selective ligand for cannabinoid CB2 receptor.

2001 • 192 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

SR 141716A Acts as an Inverse Agonist to Increase Neuronal Voltage-Dependent Ca²⁺Currents by Reversal of Tonic CB1 Cannabinoid Receptor Activity

1998 • 180 citations

Novel brain-specific 5-HT4 receptor splice variants show marked constitutive activity: role of the C-terminal intracellular domain.

1999 • 178 citations

BAY36-7620: A Potent Non-Competitive mGlu1 Receptor Antagonist with Inverse Agonist Activity.

2001 • 166 citations

Point Mutation Causing Constitutive Signaling of CXCR2 Leads to Transforming Activity Similar to Kaposi’s Sarcoma Herpesvirus-G Protein-Coupled Receptor

1999 • 159 citations

Role of subunit diversity in signaling by heterotrimeric G proteins

1997 • 150 citations

Determinants of alpha 2-adrenergic receptor activation of G proteins: evidence for a precoupled receptor/G protein state.

1994 • 149 citations

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

1998 • 141 citations

Inverse agonist actions of typical and atypical antipsychotic drugs at the human 5-hydroxytryptamine(2C) receptor.

2001 • 141 citations

Human Interferon-γ–inducible Protein 10 (IP-10) Inhibits Constitutive Signaling of Kaposi's Sarcoma–associated Herpesvirus G Protein–coupled Receptor

1998 • 136 citations

Constitutive activity of histamine h(3) receptors stably expressed in SK-N-MC cells: display of agonism and inverse agonism by H(3) antagonists.

2001 • 135 citations

A constitutively active mutant beta 2-adrenergic receptor is constitutively desensitized and phosphorylated.

1994 • 129 citations

Discrete activation of transduction pathways associated with acetylcholine m1 receptor by several muscarinic ligands

1994 • 126 citations

Serotonin 5‐HT_1B and 5‐HT_1D receptors form homodimers when expressed alone and heterodimers when co‐expressed

1999 • 121 citations

Evidence that antipsychotic drugs are inverse agonists at D₂ dopamine receptors

1997 • 116 citations

Tight Association of the Human Mel_1a-Melatonin Receptor and G_i: Precoupling and Constitutive Activity

1999 • 110 citations

Use of constitutive G protein-coupled receptor activity for drug discovery.

2000 • 106 citations

Exendin-(9–39) Is an Inverse Agonist of the Murine Glucagon-Like Peptide-1 Receptor: Implications for Basal Intracellular Cyclic Adenosine 3′,5′-Monophosphate Levels and β-Cell Glucose Competence**This work was supported by Grant 31-46958.96 from the Swiss National Science Foundation (to B.T.).

1998 • 100 citations

Regulation of the Cellular Localization and Signaling Properties of the α_1B- and α_1D-Adrenoceptors by Agonists and Inverse Agonists

2000 • 95 citations

A conserved tyrosine residue (Y601) in transmembrane domain 5 of the human thyrotropin receptor serves as a molecular switch to determine G‐protein coupling

1998 • 89 citations

Signal amplification in HL‐60 granulocytes

1991 • 88 citations

Inhibition of the constitutive activity of human 5‐HT_1A receptors by the inverse agonist, spiperone but not the neutral antagonist, WAY 100,635

1997 • 86 citations

Interactions of α-Melanotropin and Agouti on B16 Melanoma Cells: Evidence for Inverse Agonism of Agouti

1997 • 85 citations

Antagonists of bradykinin that stabilize a G-protein-uncoupled state of the B2 receptor act as inverse agonists in rat myometrial cells

1994 • 83 citations

A new constitutively activating point mutation in the luteinizing hormone/choriogonadotropin receptor gene in cases of male-limited precocious puberty.

1995 • 81 citations

G proteins of the Gq family couple the H2 histamine receptor to phospholipase C.

1996 • 81 citations

Distinct Interaction of Human and Guinea Pig Histamine H₂-Receptor with Guanidine-Type Agonists

2001 • 73 citations

Mechanisms of Agonism and Inverse Agonism at Serotonin 5‐HT_1A Receptors

2000 • 59 citations

Constitutive Activity of a Chimeric D₂/D₁Dopamine Receptor

1997 • 59 citations

Constitutive activity of human prostaglandin E receptor EP₃ isoforms

1997 • 57 citations

Modulation of basal intracellular calcium by inverse agonists and phorbol myristate acetate in rat‐1 fibroblasts stably expressing α_1d‐adrenoceptors

1999 • 54 citations

The Luteinizing Hormone Receptor Activates Phospholipase C via Preferential Coupling to G_i2

1999 • 50 citations

Inverse agonist activities of β‐adrenoceptor antagonists in rat myocardium

1999 • 48 citations

Modulation of forskolin‐mediated adenylyl cyclase activation by constitutively active G_s‐coupled receptors

1997 • 45 citations

Unoccupied β-adrenoceptor-induced adenylyl cyclase stimulation in turkey erythrocyte membranes

1994 • 44 citations

Constitutive activation of cyclic AMP but not phosphatidylinositol signaling caused by four mutations in the 6th transmembrane helix of the human thyrotropin receptor

1994 • 44 citations

Up‐regulation of a constitutively active form of the β₂‐adrenoceptor by sustained treatment with inverse agonists but not antagonists

1996 • 41 citations

Agonist-, antagonist-, and inverse agonist-regulated trafficking of the delta-opioid receptor correlates with, but does not require, G protein activation.

2001 • 37 citations

Inverse Agonism at Dopamine D2 Receptors Haloperidol-Induced Prolactin Release from GH4C1 Cells Transfected with the Human D2 Receptor Is Antagonized by R(−)-n-propylnorapomorphine, Raclopride, and Phenoxybenzamine

1996 • 36 citations

Selective and Nonselective Inverse Agonists for Constitutively Active Type-1 Parathyroid Hormone Receptors: Evidence for Altered Receptor Conformations*

2001 • 35 citations

An Efficacy-Dependent Effect of Cardiac Overexpression of β₂-Adrenoceptor on Ligand Affinity in Transgenic Mice

1997 • 26 citations

The effect of SB-236057-A, a selective 5-HT 1B receptor inverse agonist, on in vivo extracellular 5-HT levels in the freely-moving guinea-pig

2000 • 24 citations

Gα‐16 complements the signal transduction cascade of chemotactic receptors for complement factor C5a (C5a‐R) and N‐formylated peptides (fMLF‐R) in Xenopus laevis oocytes: Gα‐16 couples to chemotactic receptors in Xenopus oocytes

1995 • 16 citations

Differential activation of dibutyryl cAMP-differentiated HL-60 human leukemia cells by chemoattractants

1994 • 14 citations