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Author Correction: PRESTO-Tango as an open-source resource for interrogation of the druggable human GPCRome
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Article
Structure, function and pharmacology of human itch GPCRs
The MRGPRX family of receptors (MRGPRX1–4) is a family of mas-related G-protein-coupled receptors that have evolved relatively recently1. Of these, MRGPRX2 and MRGPRX4 are key physiological and pathological media...
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Article
In silico design of novel probes for the atypical opioid receptor MRGPRX2
High-throughput screening identifies opioid compounds and prodynorphin-derived peptide agonists of the G-protein-coupled receptor MRGPRX2 and informs a homology model that is used for in silico screening to find ...
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Article
Allosteric ligands for the pharmacologically dark receptors GPR68 and GPR65
At least 120 non-olfactory G-protein-coupled receptors in the human genome are ‘orphans’ for which endogenous ligands are unknown, and many have no selective ligands, hindering the determination of their biolo...
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Article
PRESTO-Tango as an open-source resource for interrogation of the druggable human GPCRome
Roth and colleagues have developed PRESTO-Tango, a new open-source platform for high-throughput screening of the entire human nonolfactory GPCRome, and they show how it can be used to identify new ligands for ...
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Article
The Presynaptic Component of the Serotonergic System is Required for Clozapine's Efficacy
Clozapine, by virtue of its absence of extrapyramidal side effects and greater efficacy, revolutionized the treatment of schizophrenia, although the mechanisms underlying this exceptional activity remain contr...
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Article
Deorphanization of Novel Peptides and Their Receptors
Peptide hormones and neuropeptides play important roles in endocrine and neural signaling, often using G protein-coupled receptor (GPCR)-mediated signaling pathways. However, the rate of novel peptide discover...
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Chapter
Molecular Biology and Genomic Organization of G Protein-Coupled Serotonin Receptors
Among animals with nervous systems, serotonin (5-hydroxytryptamine; 5-HT) is a ubiquitous neurotransmitter, and numerous classes and subclasses of G protein-coupled 5-HT receptors have evolved to transduce ext...
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Article
Fast dissociation rates predict neither efficacy nor lack of side-effects
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Article
Magic shotguns versus magic bullets: selectively non-selective drugs for mood disorders and schizophrenia
Most common central nervous system disorders — such as depression, bipolar disorder and schizophrenia — seem to be polygenic in origin, and the most effective medications have exceedingly complex pharmacologie...
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Article
Reply: H1-histamine Receptor Affinity Predicts Short-term Weight Gain for Typical and Atypical Antipsychotic Drugs
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Article
H1-Histamine Receptor Affinity Predicts Short-Term Weight Gain for Typical and Atypical Antipsychotic Drugs
As a result of superior efficacy and overall tolerability, atypical antipsychotic drugs have become the treatment of choice for schizophrenia and related disorders, despite their side effects. Weight gain is a...