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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DREADDs for neuroscientists

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G Protein-Coupled Receptors as Targets for Approved Drugs: How Many Targets and How Many Drugs?

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Structure-Function of the G Protein–Coupled Receptor Superfamily

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PRESTO-Tango as an open-source resource for interrogation of the druggable human GPCRome

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Structural Features for Functional Selectivity at Serotonin Receptors

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Drug–target interaction prediction: databases, web servers and computational models

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Common activation mechanism of class A GPCRs

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Pharmacogenomics of GPCR Drug Targets

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How Ligands Illuminate GPCR Molecular Pharmacology

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Current Concepts and Treatments of Schizophrenia

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Allosteric sodium in class A GPCR signaling

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Chemogenetic Tools to Interrogate Brain Functions

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Structure and function of serotonin G protein-coupled receptors

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Discovery of β-Arrestin–Biased Dopamine D 2 Ligands for Probing Signal Transduction Pathways Essential for Antipsychotic Efficacy

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Reward circuitry dysfunction in psychiatric and neurodevelopmental disorders and genetic syndromes: animal models and clinical findings

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In silico design of novel probes for the atypical opioid receptor MRGPRX2

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Psychedelics as anti-inflammatory agents

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BitterDB: a database of bitter compounds

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Regulation of immune responses by tuft cells

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Serotonin receptors and heart valve disease—It was meant 2B

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Systems pharmacology in drug discovery and therapeutic insight for herbal medicines

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Development of allosteric modulators of GPCRs for treatment of CNS disorders

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The G Protein–Biased κ-Opioid Receptor Agonist RB-64 Is Analgesic with a Unique Spectrum of Activities In Vivo

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Structural determinants of 5-HT2B receptor activation and biased agonism

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The promiscuous binding of pharmaceutical drugs and their transporter-mediated uptake into cells: what we (need to) know and how we can do so

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Distinct cortical and striatal actions of a β-arrestin–biased dopamine D2 receptor ligand reveal unique antipsychotic-like properties

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On the origins of drug polypharmacology

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Low Affinity GPCRs for Metabolic Intermediates: Challenges for Pharmacologists

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Identification of a Conformational Equilibrium That Determines the Efficacy and Functional Selectivity of the μ‐Opioid Receptor

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Finding novel pharmaceuticals in the systems biology era using multiple effective drug targets, phenotypic screening and knowledge of transporters: where drug discovery went wrong and how to fix it

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Methods for the Elucidation of Protein-Small Molecule Interactions

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Lorcaserin and pimavanserin: emerging selectivity of serotonin receptor subtype–targeted drugs

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Pharmacosynthetics: Reimagining the pharmacogenetic approach

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GPCRs: Lipid-Dependent Membrane Receptors That Act as Drug Targets

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Biased Agonism at G Protein‐Coupled Receptors: The Promise and the Challenges—A Medicinal Chemistry Perspective

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Structure-Based Ligand Discovery Targeting Orthosteric and Allosteric Pockets of Dopamine Receptors

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DREADD: A Chemogenetic GPCR Signaling Platform

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DREADDs: novel tools for drug discovery and development

Lee, H.-M., Giguère, P. M., & Roth, B. L. (2013) · Drug Discovery Today · doi:10.1016/j.drudis.2013.10.018 · Cited by 97

“Selective” serotonin 5-HT2A receptor antagonists

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Hypothalamic UDP Increases in Obesity and Promotes Feeding via P2Y6-Dependent Activation of AgRP Neurons

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Dissecting the Role of Subtypes of Gastrointestinal Vagal Afferents

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Integrated Approaches for Genome-wide Interrogation of the Druggable Non-olfactory G Protein-coupled Receptor Superfamily

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Accelerated structure-based design of chemically diverse allosteric modulators of a muscarinic G protein-coupled receptor

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Antagonist Functional Selectivity: 5-HT2A Serotonin Receptor Antagonists Differentially Regulate 5-HT2A Receptor Protein Level In Vivo

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Drug Repurposing Is a New Opportunity for Developing Drugs against Neuropsychiatric Disorders

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Understanding Membrane Protein Drug Targets in Computational Perspective

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Allosteric modulators targeting CNS muscarinic receptors

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Toward G protein-coupled receptor structure-based drug design using X-ray lasers

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Emerging Roles for MAS-Related G Protein-Coupled Receptor-X2 in Host Defense Peptide, Opioid, and Neuropeptide-Mediated Inflammatory Reactions

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Irving Page Lecture: 5-HT2A serotonin receptor biology: Interacting proteins, kinases and paradoxical regulation

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How Do Molecular Dynamics Data Complement Static Structural Data of GPCRs

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CNIH4 Interacts with Newly Synthesized GPCR and Controls Their Export from the Endoplasmic Reticulum

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The CCK(-like) receptor in the animal kingdom: Functions, evolution and structures

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Split protein biosensor assays in molecular pharmacological studies

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The role of P2Y receptors in regulating immunity and metabolism

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Identification of Similar Binding Sites to Detect Distant Polypharmacology

Jalencas, X., & Mestres, J. (2013) · Molecular Informatics · doi:10.1002/minf.201300082 · Cited by 57

G protein-coupled receptors as therapeutic targets for multiple sclerosis

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Biased agonism at kappa opioid receptors: Implication in pain and mood disorders

Dogra, S., & Yadav, P. N. (2015) · European Journal of Pharmacology · doi:10.1016/j.ejphar.2015.07.018 · Cited by 54

The GTPase Rab43 Controls the Anterograde ER-Golgi Trafficking and Sorting of GPCRs

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Visualization and Quantitative Analysis of G Protein-Coupled Receptor−β-Arrestin Interaction in Single Cells and Specific Organs of Living Mice Using Split Luciferase Complementation

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Bioluminescence imaging of G protein-coupled receptor activation in living mice

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The involvement of purinergic signalling in obesity

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Recent Insights from Molecular Dynamics Simulations for G Protein-Coupled Receptor Drug Discovery

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Chemogenetics—A Transformational and Translational Platform

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Expanding the horizons of G protein-coupled receptor structure-based ligand discovery and optimization using homology models

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Expanding biological space coverage enhances the prediction of drug adverse effects in human using in vitro activity profiles

Huang, R., Xia, M., Sakamuru, S., Zhao, J., Lynch, C., Zhao, T., Zhu, H., Austin, C. P., & Simeonov, A. M. (2018) · Scientific Reports · doi:10.1038/s41598-018-22046-w · Cited by 47

Expression of Olfactory Signaling Genes in the Eye

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Excitements and Challenges in GPCR Oligomerization: Molecular Insight from FRET

Chakraborty, H., & Chattopadhyay, A. (2014) · ACS Chemical Neuroscience · doi:10.1021/cn500231d · Cited by 42

Pharmacological fingerprint of antipsychotic drugs at the serotonin 5-HT2A receptor

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Deep Learning Dynamic Allostery of G-Protein-Coupled Receptors

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GPCR structure, function, drug discovery and crystallography: report from Academia-Industry International Conference (UK Royal Society) Chicheley Hall, 1–2 September 2014

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Examining the role of mu opioid receptor endocytosis in the beneficial and side-effects of prolonged opioid use: From a symposium on new concepts in mu-opioid pharmacology

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The GPR17 receptor-A promising goal for therapy and a potential marker of the neurodegenerative process in multiple sclerosis

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Troubleshooting and deconvoluting label-free cell phenotypic assays in drug discovery

Ye, F. (2013) · Journal of Pharmacological and Toxicological Methods · doi:10.1016/j.vascn.2013.01.004 · Cited by 38

Modeling of Human Prokineticin Receptors: Interactions with Novel Small-Molecule Binders and Potential Off-Target Drugs

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Orphan Receptor GPR88 as an Emerging Neurotherapeutic Target

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QR code model: a new possibility for GPCR phosphorylation recognition

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Discovery of GPCR ligands for probing signal transduction pathways

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Marine fungal metabolite butyrolactone I prevents cognitive deficits by relieving inflammation and intestinal microbiota imbalance on aluminum trichloride-injured zebrafish

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Crystallization chaperone strategies for membrane proteins

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Tango assay for ligand-induced GPCR–β-arrestin2 interaction

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A focus on CXCR4 in Alzheimer's disease

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Towards the miniaturization of GPCR-based live-cell screening assays

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Constitutive Activities in the Thyrotropin Receptor

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Opioid toxicity: histamine, hypersensitivity, and MRGPRX2

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Conformational Ensembles in GPCR Activation

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Recent Trends and Future Prospects in Computational GPCR Drug Discovery: From Virtual Screening to Polypharmacology

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Designing, docking and molecular dynamics simulation studies of novel cloperastine analogues as anti-allergic agents: homology modeling and active site prediction for the human histamine H1 receptor

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Label-free functional assays of chemical receptors using a bioengineered cell-based biosensor with localized extracellular acidification measurement

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Advances in Dopamine D1 Receptor Ligands for Neurotherapeutics

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Selective Manipulation of Neural Circuits

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Tuning up the right signal: chemical and genetic approaches to study GPCR functions

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