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

p90 Ribosomal S6 Kinase 2, a Novel GPCR Kinase, Is Required for Growth Factor-Mediated Attenuation of GPCR Signaling

(2010) Ryan T. Strachan et al.   BIOCHEMISTRY

Prediction and Evaluation of Protein Farnesyltransferase Inhibition by Commercial Drugs

(2010) Amanda J. DeGraw et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

(2010) Shuyun Dong et al.   Nature Protocols

Structure-Based Design, Synthesis, and Biochemical and Pharmacological Characterization of Novel Salvinorin A Analogues as Active State Probes of the κ-Opioid Receptor

(2009) Feng Yan et al.   BIOCHEMISTRY

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

(2009) Ralf Heilker et al.   DRUG DISCOVERY TODAY

hERG-related drug toxicity and models for predicting hERG liability and QT prolongation

(2009) Emanuel Raschi et al.   Expert Opinion on Drug Metabolism & Toxicology

Structural Determinants of G-protein α Subunit Selectivity by Regulator of G-protein Signaling 2 (RGS2)

(2009) Adam J. Kimple et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

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

(2009) Jordi Mestres et al.   Molecular BioSystems

Genetic Deletion of p90 Ribosomal S6 Kinase 2 Alters Patterns of 5-Hydroxytryptamine2A Serotonin Receptor Functional Selectivity

(2009) R. T. Strachan et al.   MOLECULAR PHARMACOLOGY

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

(2009) X.-P. Huang et al.   MOLECULAR PHARMACOLOGY

Predicting promiscuity

(2009) Andrew L. Hopkins   NATURE

Predicting new molecular targets for known drugs

(2009) Michael J. Keiser et al.   NATURE

Molecular Mechanisms of Action and In Vivo Validation of an M4 Muscarinic Acetylcholine Receptor Allosteric Modulator with Potential Antipsychotic Properties

(2009) Katie Leach et al.   NEUROPSYCHOPHARMACOLOGY

Structure-based discovery of  2-adrenergic receptor ligands

(2009) P. Kolb et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

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

(2009) P. Jeffrey Conn et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Conciliating binding efficiency and polypharmacology

(2009) Jordi Mestres et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Novel Genetically Encoded Biosensors Using Firefly Luciferase

(2008) Frank Fan et al.   ACS Chemical Biology

Cell-based assays in GPCR drug discovery

(2008) Sandra Siehler   Biotechnology Journal

Anatomical Profiling of G Protein-Coupled Receptor Expression

(2008) Jean B. Regard et al.   CELL

Functional Selectivity in GPCR Modulator Screening

(2008) Terry Kenakin   COMBINATORIAL CHEMISTRY & HIGH THROUGHPUT SCREENING

High Throughput Screening for Orphan and Liganded GPCRs

(2008) Shou-Hua Xiao et al.   COMBINATORIAL CHEMISTRY & HIGH THROUGHPUT SCREENING

Quantifying the Relationships among Drug Classes

(2008) Jérôme Hert et al.   Journal of Chemical Information and Modeling

Novel Selective Allosteric Activator of the M1 Muscarinic Acetylcholine Receptor Regulates Amyloid Processing and Produces Antipsychotic-Like Activity in Rats

(2008) C. K. Jones et al.   JOURNAL OF NEUROSCIENCE

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

(2008) W. J. Thomsen et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Functional Assays as Prismatic Views of Drug Activity: Relevance to New Drug Discovery

(2008) TERRY KENAKIN   JOURNAL OF RECEPTORS AND SIGNAL TRANSDUCTION

Network pharmacology: the next paradigm in drug discovery

(2008) Andrew L Hopkins   Nature Chemical Biology

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

(2008) Malin C. Lagerström et al.   NATURE REVIEWS DRUG DISCOVERY

Insights into the regulation of 5-HT2A serotonin receptors by scaffolding proteins and kinases

(2008) John A. Allen et al.   NEUROPHARMACOLOGY

Opportunities and Challenges of Psychiatric Drug Discovery: Roles for Scientists in Academic, Industry and Government Settings

(2008) P Jeffrey Conn et al.   NEUROPSYCHOPHARMACOLOGY

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

(2008) Steven R. Smith et al.   Obesity

Antagonism of dopamine D2 receptor/ -arrestin 2 interaction is a common property of clinically effective antipsychotics

(2008) B. Masri et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Environmental Studies of Schizophrenia Through the Prism of Epigenetics

(2008) G. Oh et al.   SCHIZOPHRENIA BULLETIN

The 2.6 Angstrom Crystal Structure of a Human A2A Adenosine Receptor Bound to an Antagonist

(2008) V.-P. Jaakola et al.   SCIENCE

Heterotrimeric G-proteins: a short history

(2006) Graeme Milligan et al.   BRITISH JOURNAL OF PHARMACOLOGY