October 2022 "Biased G protein-coupled receptor (GPCR) ligands, which preferentially activate G protein

October 2022 "G protein-coupled receptors (GPCRs) are important drug targets characterized by a canonical impact of binding of agonists and antagonist/inverse agonists to selected structures of cannabinoid receptor 1 (CB1R), β2 adrenergic receptor (β2 AR) and A2A adenosine receptor (A2A AR). " Read more at the source

Currently, attention was mainly paid to biased signaling modulators targeting G protein-coupled receptors The biased signaling modulation of non-GPCR receptors has yet to be exploited. Toll-like receptor 4 (TLR4) is one such non-GPCR receptor, which involves MyD88-dependent and TRIF-dependent Small molecules biasedly modulating the TLR4 signaling axis not only provide probes to fine-tune receptor modulators of TLR4 would provide insight for the future development of biased modulators for other non-GPCR receptors

October 2022 "G protein-coupled receptors (GPCRs) play critical roles in human physiology and are one allosteric sites and significantly enhanced our understanding of how allosteric ligands interact with receptors structures in complex with small-molecule allosteric ligands in terms of the location of allosteric pockets, receptor-ligand

Constitutive, Basal, and β-Alanine-Mediated Activation of the Human Mas-Related G Protein-Coupled Receptor Induces Release of the Inflammatory Cytokine IL-6 and Is Dependent on NF-κB Signaling G protein-coupled receptors Members of the Mas-related G protein coupled receptors (MRGPRs), a subfamily of GPCRs, are largely expressed However, involvement of the human Mas-related G-protein coupled receptor D (MRGPRD) in the regulation

transcriptomics and peptidomics of central nervous system identify neuropeptides and their G protein-coupled receptors Neuropeptides and their specific receptors (primarily G protein-coupled receptors, GPCRs) regulate multiple

CNVs is located on chromosome 4q13.1 in the region of the gene encoding for adhesion G protein-coupled receptor

Recurrent high-impact mutations at cognate structural positions in class A G protein-coupled receptors expressed in tumors G protein-coupled receptors (GPCRs) are the largest family of human proteins. Because there are many more GPCRs than effectors, mutations in different receptors could perturb signaling but rather that cognate mutations with similar effects on GPCR function are distributed across many receptors We also discovered that no single receptor drives this pattern, but rather multiple receptors contain

via enhancing NLRP3 inflammasome activation in macrophages "The putative medium-chain free fatty acid receptor GPR84 is a G protein-coupled receptor primarily expressed in myeloid cells that constitute the innate

In 2008 (and for the first time in the clinic), the therapeutic benefits of the β-adrenergic receptor

September 2022 "GPCRs are the most potential targets for drug discovery, however, their role in oncology is underappreciated and GPCR-based anti-cancer drug is not fully investigated. Herein, we identified GPR108, a GPCR protein described in innate immune system, is a potential therapeutic target of cancer. Depletion of GPR108 dramatically inhibited the survival of various cancers. Notably, TNFα activation of NF-κB was totally impaired after GPR108 knockout. We identified gambogic acid (GA), a natural prenylated xanthone, selectively targeting GPR108. Importantly, GA engaged with GPR108 and promoted its degradation, knockout of GPR108 remarkably blocked GA inhibition of NF-κB signaling. Furthermore, in vitro and in vivo assays demonstrated that GA was dependent on GPR108 to exert anti-cancer activity. Overall, our findings supported GPR108 as a promising therapeutic target of cancer, and provided a small molecule inhibitor GA directly and selectively targeting GPR108 for cancer therapy." Read more at the source #DrGPCR #GPCR #IndustryNews

September 2022 "GPCR signaling and function depend on their associated proteins and subcellular locations. Besides G-proteins and β-arrestins, 14-3-3 proteins participate in GPCR trafficking and signaling, and they connect a large number of diverse proteins to form signaling networks. Multiple 14-3-3 isoforms exist, and a GPCR can differentially interact with different 14-3-3 isoforms in response to agonist treatment. We found that some agonist-induced GPCR/14-3-3 signal intensities can rapidly decrease. We confirmed that this phenomenon of rapidly decreasing agonist-induced GPCR/14-3-3 signal intensity could also be paralleled with GPCR/β-arrestin-2 signals, indicating diminished levels of GPCR/signal adaptor complexes during endocytosis. The temporal signals could implicate either GPCR/14-3-3 complex dissociation or the complex undergoing a degradation process. Furthermore, we found that certain GPCR ligands can regulate GPCR/14-3-3 signals temporally, suggesting a new approach for GPCR drug development by modulating GPCR/14-3-3 signals temporally." Read more at the source #DrGPCR #GPCR #IndustryNews

it contributes to pathophysiology, which is likely due to complex interactions among neuropeptides, receptor

This communication involves the ligand-mediated control of cell surface receptors that then direct their has been placed on the ability of these therapeutics to modulate diseases by acting at cell surface receptors GPCR superstructures, termed receptorsomes, both at the cell surface membrane and in the intracellular domain

validation of recombinant protein standards for quantitative Western blot analysis of cannabinoid CB1 receptor assays with antibody-antigen interaction-based approaches for quantitative analysis of G protein-coupled receptor GPCRs in general and cannabinoid CB1 receptor in particular show a progressive tendency to aggregate context due to the low solubility that the hydrophobic nature imprinted by their seven transmembrane domains Estimated values of CB1 receptor density obtained by quantitative Western blot were of the same order

critical components of the intracellular signaling pathways that mediate the effects of G protein-coupled receptors selective for certain GPCRs, as a proof RGS4 which is expressed in the brain, has been shown to modulate dopamine signaling by specifically regulating the activity of the dopamine D2 receptor; enhancing the activity of the G protein that is coupled to the receptor and leading to a decrease in dopamine signaling[4, Zhuang, Y., et al., Structural insights into the human D1 and D2 dopamine receptor signaling complexes

GPCR contributor article Canonical chemokine receptors as scavenging “decoys” Shivani Sachdev, Brendan Bouvier, Jana Selent, et al. for their study on G protein-specific mechanisms in the serotonin 5-HT2A receptor function, impacting synaptic transmission Orphan receptor GPR88 as a potential therapeutic target for PC12 cells 17-β-estradiol potentiates the neurotrophic and neuroprotective effects mediated by the dopamine D3/acetylcholine nicotinic receptor heteromer in dopaminergic neurons A new GRAB sensor reveals differences

spectroscopy to characterize ligand interactions with cell surface membrane proteins such as G-protein coupled receptors (GPCRs) and receptor tyrosine kinases. delineation of ligands involved in binding, ligand bound-state conformational determination, evaluation of receptor structuring and dynamics, and inference of distance constraints characteristic of the ligand-receptor

CXV: The Class F of G Protein-Coupled Receptors Yusman Manchanda , Dr. the therapeutic prospects of EGFR inhibition in rotenone-mediated parkinsonism in rats: Modulation of dopamine D3 receptor Molecular insights into orphan G protein-coupled receptors relevant to schizophrenia Single Unravelling G protein-coupled receptor signalling networks using global phosphoproteomics Reviews, GPCRs CXV: The Class F of G Protein-Coupled Receptors Structural and Molecular Insights into GPCR Function

August 2022 "The apelin receptor (APJ) is a target for cardiovascular indications.

GPCRs in Cardiology, Endocrinology, and Taste G-protein coupled receptor 19 (GPR19) knockout mice display Neurotensin receptor 1-biased ligand attenuates neurotensin-mediated excitation of ventral tegmental area dopamine neurons and dopamine release in the nucleus accumbens. Methods & Updates in GPCR Research Activity Map and Transition Pathways of G Protein-Coupled Receptor Computational insights into ligand-induced G protein and β-arrestin signaling of the dopamine D1 receptor

October 2022 "Background: Uncoupling proteins (UCPs) are unpaired electron carriers that uncouple oxygen intake by the electron transport chain from ATP production in the inner membrane of the mitochondria. The physiological activities of UCPs have been hotly contested, and the involvement of UCPs in the pathogenesis and progression of diabetes mellitus is among the greatest concerns. UCPs are hypothesised to be triggered by superoxide and then reduce mitochondrial free radical production, potentially protecting diabetes mellitus patients who are experiencing oxidative stress. Objectives: The objectives of the study are to find out the newest ways to treat diabetes mellitus through protein uncoupling." Read more at the source #DrGPCR #GPCR #IndustryNews

October 2022 "The activity of dopamine neurons is dependent on both intrinsic properties and afferent , D2 and GABAB receptors. Each of these receptors activates G protein-coupled inwardly rectifying potassium (GIRK) channels. KEY POINTS: Inhibitory D2 and GABAB receptors modulate dopamine neuron activity through shared G protein-coupled in the context of other G protein-coupled receptors."

Adhesion GPCRs Amelioration of non-alcoholic fatty liver disease by targeting adhesion G protein-coupled receptor of the glucagon receptor is dynamic Ligand recognition and G protein coupling of the human itch receptor 1-biased ligand attenuates neurotensin-mediated excitation of ventral tegmental area dopamine neurons and dopamine release in the nucleus accumbens Understanding the Molecular Regulation of Serotonin Receptor Insights into GPCR Function A method for structure determination of GPCRs in various states Apelin receptor

includes congrats to: Junyi Liang, Niña Caculitan, and Adam W Smith for their research on β2-adrenergic receptor restoration of tension in epithelial cells Profiling the proximal proteome of the activated μ-opioid receptor the therapeutic prospects of EGFR inhibition in rotenone-mediated parkinsonism in rats: Modulation of dopamine D3 receptor Satellite glial GPR37L1 and its ligand maresin 1 regulate potassium channel signaling and in human cancer cells [Inhibitory effect of downregulating G protein-coupled receptor class C group

GPCR Activation and Signaling Coupling between GPR143 and dopamine D2 receptor is required for selective potentiation of dopamine D2 receptor function by L-3,4-dihydroxyphenylalanine in the dorsal striatum Impact of membrane lipid polyunsaturation on dopamine D2 receptor ligand binding and signaling GPCR Binders Gαi-derived peptide binds the µ-opioid receptor. A growing understanding of the role of muscarinic receptors in the molecular pathology and treatment

Transmembrane domains of GPCR dimers – a novel hot spot for drug discovery G-protein-coupled receptors domain (TMD), with the most compelling studies revealing that the transmembrane helices TM4 and TM5 activation, desensitization and trafficking is the apelin receptor (APJ) (Y. as with bradykinin 1 and 2 receptors (B. dimer formation, where the dimer corresponds to the biased receptor.

development of its best-in-class and first-in-class immuno-oncology programs STRASBOURG, France & MONTREAL- Domain company specializing in the research and development of innovative drugs targeting G Protein-Coupled Receptors