Strategies to Discover Unexpected Targets for Drugs Active at G Protein–Coupled Receptors

The sequence of the human genome

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TGF-β SIGNAL TRANSDUCTION

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Crystal Structure of Rhodopsin: A G Protein-Coupled Receptor

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The druggable genome

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High-Resolution Crystal Structure of an Engineered Human β 2 -Adrenergic G Protein–Coupled Receptor

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The G-Protein-Coupled Receptors in the Human Genome Form Five Main Families. Phylogenetic Analysis, Paralogon Groups, and Fingerprints

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Relating protein pharmacology by ligand chemistry

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Opiate Receptor: Demonstration in Nervous Tissue

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Evolving the lock to fit the key to create a family of G protein-coupled receptors potently activated by an inert ligand

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Evolving Concepts in G Protein-Coupled Receptor Endocytosis: The Role in Receptor Desensitization and Signaling

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The 2.6 Angstrom Crystal Structure of a Human A 2A Adenosine Receptor Bound to an Antagonist

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Predicting new molecular targets for known drugs

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Valvular heart disease associated with fenfluramine-phentermine

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Structural diversity of G protein-coupled receptors and significance for drug discovery

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β-Arrestins and Cell Signaling

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Clozapine Treatment for Suicidality in Schizophrenia<subtitle>International Suicide Prevention Trial (InterSePT)</subtitle>

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Hallucinogens

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Magic shotguns versus magic bullets: selectively non-selective drugs for mood disorders and schizophrenia

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The Orphan G Protein-coupled Receptor GPR40 Is Activated by Medium and Long Chain Fatty Acids

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G-protein-coupled receptors and signaling networks: emerging paradigms

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Role of β-Arrestin in Mediating Agonist-Promoted G Protein-Coupled Receptor Internalization

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Aripiprazole, A Novel Atypical Antipsychotic Drug with a Unique and Robust Pharmacology

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G Protein-Coupled Receptor Allosterism and Complexing

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Valvular Heart Disease and the Use of Dopamine Agonists for Parkinson's Disease

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H1-Histamine Receptor Affinity Predicts Short-Term Weight Gain for Typical and Atypical Antipsychotic Drugs

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Salvinorin A: A potent naturally occurring nonnitrogenous κ opioid selective agonist

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The G protein-coupled receptor repertoires of human and mouse

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β-Arrestin-dependent, G Protein-independent ERK1/2 Activation by the β2 Adrenergic Receptor

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Evidence for Possible Involvement of 5-HT _2B Receptors in the Cardiac Valvulopathy Associated With Fenfluramine and Other Serotonergic Medications

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Dopamine Agonists and the Risk of Cardiac-Valve Regurgitation

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Anatomical Profiling of G Protein-Coupled Receptor Expression

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The genetic design of signaling cascades to record receptor activation

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Molecular mechanisms of ligand binding, signaling, and regulation within the superfamily of G-protein-coupled receptors: molecular modeling and mutagenesis approaches to receptor structure and function

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Genome Scan Meta-Analysis of Schizophrenia and Bipolar Disorder, Part III: Bipolar Disorder

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Opiate Agonists and Antagonists Discriminated by Receptor Binding in Brain

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Heterotrimeric G‐proteins: a short history

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Drugs and Valvular Heart Disease

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Can we rationally design promiscuous drugs?

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Fluorescent indicators of cAMP and Epac activation reveal differential dynamics of cAMP signaling within discrete subcellular compartments

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Possible Role of Valvular Serotonin 5-HT2B Receptors in the Cardiopathy Associated with Fenfluramine

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

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Function of the serotonin 5-hydroxytryptamine 2B receptor in pulmonary hypertension

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A β-Arrestin/Green Fluorescent Protein Biosensor for Detecting G Protein-coupled Receptor Activation

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Evolution of Key Cell Signaling and Adhesion Protein Families Predates Animal Origins

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Lorcaserin, a Novel Selective Human 5-Hydroxytryptamine2C Agonist: in Vitro and in Vivo Pharmacological Characterization

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G-protein-coupled receptors at a glance

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Finding the Intracellular Signaling Pathways Affected by Mood Disorder Treatments

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Biochemical and pharmacological control of the multiplicity of coupling at G-protein-coupled receptors

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Pharmacology and physiology of human adrenergic receptor polymorphisms

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3,4-Methylenedioxymethamphetamine (MDMA, “Ecstasy”) Induces Fenfluramine-Like Proliferative Actions on Human Cardiac Valvular Interstitial Cells in Vitro

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Salbutamol: a new, selective β‐adrenoceptive receptor stimulant

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Structure-based discovery of β 2 -adrenergic receptor ligands

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Subtype-selective allosteric modulators of muscarinic receptors for the treatment of CNS disorders

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Salvia divinorum and salvinorin A: new pharmacologic findings

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Novel Selective Allosteric Activator of the M1Muscarinic Acetylcholine Receptor Regulates Amyloid Processing and Produces Antipsychotic-Like Activity in Rats

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Control of Yeast Mating Signal Transduction by a Mammalian β 2 -adrenergic Receptor and G s α Subunit

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Novel Genetically Encoded Biosensors Using Firefly Luciferase

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Chimeric G Proteins Allow a High-Throughput Signaling Assay of Gi-Coupled Receptors

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Salvinorin A, an Active Component of the Hallucinogenic Sage Salvia divinorum Is a Highly Efficacious κ-Opioid Receptor Agonist: Structural and Functional Considerations

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The topology of drug–target interaction networks: implicit dependence on drug properties and target families

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The Identification of Ligands at Orphan G-Protein Coupled Receptors

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Lorcaserin (APD356), a Selective 5‐HT2CAgonist, Reduces Body Weight in Obese Men and Women

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Seven-Transmembrane Receptor Signaling Through β-Arrestin

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High-Throughput Screening of G Protein-Coupled Receptor Antagonists Using a Bioluminescence Resonance Energy Transfer 1-Based β-Arrestin2 Recruitment Assay

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The pipeline and future of drug development in schizophrenia

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Is Gα16 the optimal tool for fishing ligands of orphan G-protein-coupled receptors?

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Predicting promiscuity

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Evidence for a Model of Agonist-induced Activation of 5-Hydroxytryptamine 2A Serotonin Receptors That Involves the Disruption of a Strong Ionic Interaction between Helices 3 and 6

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Quantifying the Relationships among Drug Classes

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Ethnopharmacology of ska María Pastora (Salvia divinorum, Epling AND Játiva-M.)

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A historical perspective of clozapine.

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Salvinorin A: the ‘magic mint’ hallucinogen finds a molecular target in the kappa opioid receptor

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G-protein-coupled receptor-focused drug discovery using a target class platform approach

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Parallel Functional Activity Profiling Reveals Valvulopathogens Are Potent 5-Hydroxytryptamine2B Receptor Agonists: Implications for Drug Safety Assessment

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G Protein Selectivity Is Regulated by Multiple Intracellular Regions of GPCRs

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Directed molecular evolution of DREADDs: a generic approach to creating next-generation RASSLs

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Antinociceptive profile of salvinorin A, a structurally unique kappa opioid receptor agonist

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Overexpression of the α1B-adrenergic receptor causes apoptotic neurodegeneration: Multiple system atrophy

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The highly efficacious actions of N-desmethylclozapine at muscarinic receptors are unique and not a common property of either typical or atypical antipsychotic drugs: is M1 agonism a pre-requisite for mimicking clozapine?s actions?

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G-protein-coupled receptors in Saccharomyces cerevisiae: high-throughput screening assays for drug discovery

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Withdrawal of Vioxx Casts a Shadow Over COX-2 Inhibitors

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Orphan GPCR research

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