Inverse agonism and the regulation of receptor number

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

1993 • 1,213 citations

Constitutive activity of receptors coupled to guanine nucleotide regulatory proteins

1993 • 769 citations

Enhanced Myocardial Function in Transgenic Mice Overexpressing the β ₂ -Adrenergic Receptor

1994 • 745 citations

Human herpesvirus KSHV encodes a constitutively active G-protein-coupled receptor linked to cell proliferation

1997 • 664 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

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

1989 • 519 citations

Ligand-regulated internalization and recycling of human beta 2-adrenergic receptors between the plasma membrane and endosomes containing transferrin receptors.

1992 • 445 citations

Physiological effects of inverse agonists in transgenic mice with myocardial overexpression of the β2-adrenoceptor

1995 • 408 citations

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

1996 • 377 citations

Inverse agonist activity of beta-adrenergic antagonists.

1994 • 357 citations

The dynamic role of palmitoylation in signal transduction

1995 • 315 citations

Structural Instability of a Constitutively Active G Protein-coupled Receptor

1997 • 285 citations

Inverse agonism: pharmacological curiosity or potential therapeutic strategy?

1995 • 285 citations

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

1994 • 261 citations

Constitutively active 5-hydroxytryptamine2C receptors reveal novel inverse agonist activity of receptor ligands.

1994 • 249 citations

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

1996 • 235 citations

Negative antagonists promote an inactive conformation of the beta 2-adrenergic receptor.

1994 • 224 citations

Internal Trafficking and Surface Mobility of a Functionally Intact β₂-Adrenergic Receptor-Green Fluorescent Protein Conjugate

1997 • 220 citations

Antagonist-stimulated internalization of the G protein-coupled cholecystokinin receptor.

1997 • 198 citations

Constitutive activation of a single effector pathway: evidence for multiple activation states of a G protein-coupled receptor.

1996 • 188 citations

β2-Adrenergic Receptor Desensitization, Internalization, and Phosphorylation in Response to Full and Partial Agonists

1997 • 156 citations

From ligand binding to gene expression: new insights into the regulation of G-protein-coupled receptors

1992 • 143 citations

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

1994 • 129 citations

Coupling efficiencies of human alpha 1-adrenergic receptor subtypes: titration of receptor density and responsiveness with inducible and repressible expression vectors.

1996 • 122 citations

Agonist regulation of cellular G protein levels and distribution: mechanisms and functional implications

1993 • 116 citations

Evidence that antipsychotic drugs are inverse agonists at D₂ dopamine receptors

1997 • 116 citations

Thrombin Receptors on Human Platelets

1997 • 109 citations

Two Isoforms of the Prostaglandin E Receptor EP3 Subtype Different in Agonist-independent Constitutive Activity

1996 • 106 citations

Regulation of receptor expression by agonists: transcriptional and post-transcriptional controls

1991 • 103 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

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

Constitutive activation of muscarinic receptors by the G‐protein G_q

1995 • 73 citations

Inverse agonist-induced up-regulation of the human beta2-adrenoceptor in transfected neuroblastoma X glioma hybrid cells.

1996 • 72 citations

Serotonergic antagonists differentially inhibit spontaneous activity and decrease ligand binding capacity of the rat 5-hydroxytryptamine type 2C receptor in Sf9 cells.

1995 • 69 citations

Up-regulation of the levels of expression and function of a constitutively active mutant of the hamster α1B-adrenoceptor by ligands that act as inverse agonists

1997 • 66 citations

β-Adrenergic Receptor Kinase (GRK2) Colocalizes with β-Adrenergic Receptors during Agonist-induced Receptor Internalization

1997 • 66 citations

Ligand-induced overexpression of a constitutively active β ₂ -adrenergic receptor: Pharmacological creation of a phenotype in transgenic mice

1997 • 64 citations

Silencing of the Constitutive Activity of the Dopamine D1B Receptor

1996 • 57 citations

Okadaic Acid Increases Nerve Growth Factor Secretion, mRNA Stability, and Gene Transcription in Primary Cultures of Cortical Astrocytes

1995 • 51 citations

Analysis of inverse agonism at the δ opioid receptor after expression in Rat 1 fibroblasts

1996 • 50 citations

Regulation of basal adenylate cyclase activity in neuroblastoma × glioma hybrid, NG108-15, cells transfected to express the human β 2 adrenoceptor: evidence for empty receptor stimulation of the adenylate cyclase cascade

1994 • 47 citations

The stoichiometry of expression of protein components of the stimulatory adenylyl cyclase cascade and the regulation of information transfer

1996 • 42 citations

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

1996 • 41 citations

Degradation of G11α/Gqα Is Accelerated by Agonist Occupancy of α1A/D, α1B, and α1C Adrenergic Receptors

1995 • 40 citations

Agonist regulation of adenylate cyclase activity in neuroblastoma × glioma hybrid NG108-15 cells transfected to co-express adenylate cyclase type II and the β2-adrenoceptor. Evidence that adenylate cyclase is the limiting component for receptor-mediated stimulation of adenylate cyclase activity

1996 • 39 citations

Inverse agonistic effect of ICI-174,864 on the cloned delta-opioid receptor: role of G protein and adenylyl cyclase activation.

1996 • 37 citations

Secretion of Protease Nexin-1 by C6 Glioma Cells Is under the Control of a Heterotrimeric G Protein, Go1

1996 • 33 citations

Propranolol treatment externalizes beta-adrenergic receptors in guinea pig myocardium and prevents further externalization by ischemia.

1987 • 32 citations

Signalling and regulation of the α1B-adrenergic receptor

1995 • 12 citations

A constitutively active mutant of the α1B-adrenergic receptor can cause greater agonist-dependent down-regulation of the G-proteins Gqα and G11α than the wild-type receptor

1996 • 11 citations