Constitutive activation of G protein-coupled receptors and diseases: insights into mechanisms of activation and therapeutics.
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The chemokine receptor CCR1 is constitutively active, which leads to G protein-independent, β-arrestin-mediated internalizationHow genetic errors in GPCRs affect their function: Possible therapeutic strategiesLeu128(3.43) (l128) and Val247(6.40) (V247) of CXCR1 are critical amino acid residues for g protein coupling and receptor activation.Gs-DREADD Knock-In Mice for Tissue-Specific, Temporal Stimulation of Cyclic AMP SignalingSalt bridge integrates GPCR activation with protein traffickingFemale mice expressing constitutively active mutants of FSH receptor present with a phenotype of premature follicle depletion and estrogen excessChaperoning G protein-coupled receptors: from cell biology to therapeuticsFitting the complexity of GPCRs modulation into simple hypotheses of ligand design.Histaminergic system in brain disorders: lessons from the translational approach and future perspectives.Modulation of cellular signaling by herpesvirus-encoded G protein-coupled receptors.Functional studies on twenty novel naturally occurring melanocortin-4 receptor mutations.Biased signaling in naturally occurring mutations in human melanocortin-3 receptor gene.The G-protein-coupled bile acid receptor, Gpbar1 (TGR5), negatively regulates hepatic inflammatory response through antagonizing nuclear factor κ light-chain enhancer of activated B cells (NF-κB) in micePersonalized biochemistry and biophysics.Quantifying conformational changes in GPCRs: glimpse of a common functional mechanism.Domain coupling in GPCRs: the engine for induced conformational changesThe melanocortin-4 receptor: physiology, pharmacology, and pathophysiology.Rescue of misrouted GnRHR mutants reveals its constitutive activityDifferential Virtual Screening (DVS) with Active and Inactive Molecular Models for Finding and Profiling GPCR Modulators: Case of the CCK1 Receptor.Persistent signaling by thyrotropin-releasing hormone receptors correlates with G-protein and receptor levels.Unifying view of mechanical and functional hotspots across class A GPCRs.The G-Protein-Coupled Bile Acid Receptor Gpbar1 (TGR5) Inhibits Gastric Inflammation Through Antagonizing NF-κB Signaling PathwayThe G-protein-coupled bile acid receptor Gpbar1 (TGR5) suppresses gastric cancer cell proliferation and migration through antagonizing STAT3 signaling pathwayConstitutively active ALK2 receptor mutants require type II receptor cooperationRecurrent activating mutations of G-protein-coupled receptor CYSLTR2 in uveal melanomaStructure and dynamics of a constitutively active neurotensin receptor.Inhibition of SRF/myocardin reduces aortic stiffness by targeting vascular smooth muscle cell stiffening in hypertension.Analysis of the Serotonergic System in a Mouse Model of Rett Syndrome Reveals Unusual Upregulation of Serotonin Receptor 5bNew perspectives regarding β(2) -adrenoceptor ligands in the treatment of asthma.Functional characterization and pharmacological rescue of melanocortin-4 receptor mutations identified from obese patients.The Serotonin Receptor Subtype 5b Specifically Interacts with Serotonin Receptor Subtype 1AActivation induces structural changes in the liganded angiotensin II type 1 receptor.Mutation-Induced Functional Alterations of CCR6.Cannabinoid 1 G protein-coupled receptor (periphero-)neutral antagonists: emerging therapeutics for treating obesity-driven metabolic disease and reducing cardiovascular risk.Electrostatic Interactions in Protein Structure, Folding, Binding, and Condensation.Modeling and Deorphanization of Orphan GPCRs.Pharmacoperones as Novel Therapeutics for Diverse Protein Conformational Diseases.TGR5 suppresses high glucose-induced upregulation of fibronectin and transforming growth factor-β1 in rat glomerular mesangial cells by inhibiting RhoA/ROCK signaling.Allosteric modulation as a unifying mechanism for receptor function and regulation.A focus on CXCR4 in Alzheimer's disease
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Constitutive activation of G protein-coupled receptors and diseases: insights into mechanisms of activation and therapeutics.
description
article científic
@ca
article scientifique
@fr
articolo scientifico
@it
artigo científico
@pt
bilimsel makale
@tr
scientific article published on 09 August 2008
@en
vedecký článok
@sk
vetenskaplig artikel
@sv
videnskabelig artikel
@da
vědecký článek
@cs
name
Constitutive activation of G p ...... f activation and therapeutics.
@en
Constitutive activation of G p ...... f activation and therapeutics.
@nl
type
label
Constitutive activation of G p ...... f activation and therapeutics.
@en
Constitutive activation of G p ...... f activation and therapeutics.
@nl
prefLabel
Constitutive activation of G p ...... f activation and therapeutics.
@en
Constitutive activation of G p ...... f activation and therapeutics.
@nl
P2860
P1476
Constitutive activation of G p ...... f activation and therapeutics.
@en
P2093
Ya-Xiong Tao
P2860
P304
P356
10.1016/J.PHARMTHERA.2008.07.005
P577
2008-08-09T00:00:00Z