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2022 Comparative studies of AlphaFold, RoseTTAFold and Modeller: a case study involving the use of G-protein-coupled receptors "Neural network (NN)-based protein modeling methods have improved significantly in recent G-protein-coupled receptor (GPCR) proteins are particularly interesting since they are involved in numerous This work directly compares the performance of these novel deep learning-based protein modeling methods We collected the experimentally determined structures of 73 GPCRs from the Protein Data Bank.

September 2022 "The GPR15 receptor is a G protein-coupled receptor (GPCR), which is activated by an endogenous Moreover, whether the receptor can also couple to Gs , Gq/11 and G12/13 is unclear. Gα protein signalling using a G protein activation assay and second messenger assay conducted on living The results show that the GPR15 receptor preferentially couples to Gi/o rather than other pathways in Furthermore, the GPR15 receptor signals through Gi/o to inhibit cAMP accumulation, which could be blocked

October 2022 "The cAMP-dependent protein kinase (PKA) system represents a primary cell-signaling pathway PKA facilitates the actions of hormones, neurotransmitters and other signaling molecules that bind G-protein coupled receptors (GPCR) to modulate cAMP levels. Through its control of synaptic events, exocytosis, transcriptional regulation, and more, PKA signaling Neural PKA signaling is regulated by afferent and peripheral efferent signals that link specific neural

Mutations in G protein-coupled receptors (GPCRs) underlie numerous diseases. Many cause receptor misfolding and failure to reach the cell surface. We previously demonstrated rescue of cell surface expression of luteinizing hormone receptor mutants we demonstrate that a similar approach can be employed to rescue mutant follicle-stimulating hormone receptors achieved for 6 by treatment with 1 µM CAN1404 for 24 h, and a corresponding increase in FSH-induced signaling

Excited to hear Dr. Sandra Berndt talk about new structural perspectives in GPCR-mediated Src family kinase activation. Register here (FREE) https://www.ecosystem.drgpcr.com/dr-gpcr-virtual-cafe #drgpcr #gpcr #virtualcafe

October 2022 "Over three decades of research have provided thorough insights into G protein-coupled receptor Agonist activation of the β2-adrenoceptor (β2AR) causes its S-nitrosylation that is required for the receptor Eliminating β2AR S-nitrosylation by mutation of C265 augments β2AR protein kinase A signaling, enables β2AR nitric oxide (NO) signaling, renders mice resistant to bronchoconstriction, and protects mice from

August 2022 Gαs and Gαq/11 protein coupling bias of two AVPR2 mutants (R68W and V162A) that cause nephrogenic AVPR2 is a kind of G protein coupled receptor (GPCR) and mainly couples with Gαs protein leading to cAMP the conformational change of the receptor because of the mutation and related downstream signaling. R68W showed bias to coupling with Gαq/11 protein rather than V162A and wild-type receptor. between the changed conformation of the receptor and consequently activated signaling pathways, and

October 2022 "The canonical model for G protein-coupled receptors (GPCRs) activation assumes that stimulation of heterotrimeric G protein signaling upon ligand binding occurs solely at the cell surface and that In this model, GPCR signaling is turned-off by receptor phosphorylation via GPCR kinases (GRKs) and subsequent via G proteins from endosomes. of GPCR signaling.

October 2022 "Adhesion G protein-coupled receptors (aGPCRs) are keys of many physiological events and A comparison of Gq, Gs, Gi, G12 and G13 engagements with GPR110 reveals details of G-protein engagement /G13 engage receptor mainly through hydrophobic interaction. Taken together, our study fills the missing information of GPCR/G-protein engagement and provides a framework for understanding aGPCR activation and GPR110 signaling."

this review, we will discuss the regulation of mTORC1 by upstream stimuli, with a specific focus on G-protein coupled receptor (GPCR) signaling to mTORC1.

October 2022 "Heterotrimeric G proteins couple activated G protein-coupled receptors (GPCR) to intracellular signaling pathways. of GPCR activation upon acquiring mutations that prevent GTPase activity and result in constitutive signaling YM-254890 (YM) can inhibit signaling by both GPCR-activated wild type αq and GPCR-independent αqQ209L Treatment of cells with YM failed to inhibit signaling by these PM-restricted αqQ209L.

Acquired hypocalciuric hypercalcemia (AHH) is a rare disease caused by calcium-sensing receptor (CaSR simple blocking or biased properties (i.e., stimulatory or blocking effects on different downstream signaling This emphasizes the importance of the Gi/o (pertussis toxin-sensitive G proteins, whose βγ subunits activate multiple signals, including ERK1/2) in regulating parathyroid hormone secretion. (f) the presence of CaSR autoantibodies that operated as biased allosteric modulators of CaSR, and (g)

August 2022 "Three classes of G-protein-coupled receptor (GPCR) partners - G proteins, GPCR kinases, bound to these interaction partners available today do not reveal a clear conformational basis for signaling differences in the orientation of individual residues and/or their interactions not easily detectable in the receptor-transducer

September 2022 Regulator of G Protein Signaling 20 Correlates with Long Intergenic Non-Coding RNA (lincRNAs Interestingly, RGS (Regulators of G protein signaling) proteins, which negatively regulate GPCR signaling cystadenocarcinoma: p = 0.048); (d) RGS20 was found to be significantly associated with some tumor-related signaling Our analysis further supports the putative function of RGS proteins, particularly RGS20, in cancer."

Constitutive, Basal, and β-Alanine-Mediated Activation of the Human Mas-Related G Protein-Coupled Receptor D Induces Release of the Inflammatory Cytokine IL-6 and Is Dependent on NF-κB Signaling G protein-coupled 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 through MRGPRD was investigated further by probing downstream signaling effectors along the Gαq/Phospholipase

October 2022 "Protease activated receptors (PARs) are among the first receptors shown to transactivate receptors as diverse as receptor kinases, prostanoid receptors, purinergic receptors and ionic channels We will discuss recent evidence as well as what we consider as emerging areas to explore; from the signalling and signaling pathways is only beginning to be explored and represents a novel mechanism providing diversity to receptor function and play important roles in physiology and disease."

affect processes related to perception, cognition and sensory processing mostly via the serotonin 5-HT2A receptor

Opioid receptors are G-protein-coupled receptors (GPCRs) part of cell signaling paths of direct interest low pH at tissue targeted by opioid drugs in pain management could impact drug binding to the opioid receptor , because opioid drugs typically have a protonated amino group that contributes to receptor binding, In this review, we discuss the relationship between structure, function, and dynamics of opioid receptors from the perspective of the usefulness of computational studies to evaluate protonation-coupled opioid-receptor

G protein-coupled receptors (GPCRs) transmit extracellular signals to the inside by activation of intracellular Different agonists can promote differential receptor-induced signaling responses - termed bias - potentially Here, we compared the efficacy of seven agonists to induce G protein, G protein-coupled receptor kinase However, the rank order of the agonists for G protein- and GRK2-M3R interaction was the same, suggesting that G protein and GRK2 binding to M3R requires similar receptor conformations, whereas requirements

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

October 2022 "Background: Uncoupling proteins (UCPs) are unpaired electron carriers that uncouple oxygen hypothesised to be triggered by superoxide and then reduce mitochondrial free radical production, potentially protecting Objectives: The objectives of the study are to find out the newest ways to treat diabetes mellitus through protein

and anosmia, is due to mutations in the ANOS1 gene that encodes for the extracellular matrix (ECM) protein Prokineticins (PKs) exert their biological functions through the activation of the G protein-coupled receptors (GPCRs) prokineticin receptor 1 and 2 (PKR1, 2), and mutations in the PK2 and PKR2 genes are is able to enhance the activation of the ERK1/2 (extracellular signal-regulated kinase 1/2) pathway could assist the WAP domain both in the binding to PKR2 and in the modulation of the activation of the receptor

Characterization of a new WHIM syndrome mutant reveals mechanistic differences in regulation of the chemokine receptor The S339fs5 and R334X mutants exhibited significantly increased signaling compared to wild type CXCR4 including agonist-promoted calcium flux and extracellular signal-regulated kinase activation. Interestingly, there were also significant differences in receptor degradation, with S339fs5 having a together, these studies identify a new WHIM syndrome mutant, CXCR4-S339fs5, that promotes enhanced signaling

Herein, we identified GPR108, a GPCR protein described in innate immune system, is a potential therapeutic with GPR108 and promoted its degradation, knockout of GPR108 remarkably blocked GA inhibition of NF-κB signaling

G protein-coupled receptors (GPCRs) are membrane-bound proteins that sense external stimuli and relay Bouvier, M., Oligomerization of G-protein-coupled transmitter receptors.   Graaf, C., et al., Glucagon-Like Peptide-1 and Its Class B G Protein-Coupled Receptors: A Long March induces G-protein-coupled receptor heteromer formation.   Wootten, D., et al., Allostery and Biased Agonism at Class B G Protein-Coupled Receptors.  

Emerging evidence suggests adenosine G protein-coupled receptors (GPCRs) are promising therapeutic targets The adenosine A1 and A2A receptors are expressed in the human brain and have a proposed involvement in Targeting these receptors preclinically can mitigate pathogenic β-amyloid and tau neurotoxicity whilst accessible summary of the literature on Alzheimer's disease and the therapeutic potential of A1 and A2A receptors Although there are no available medicines targeting these receptors approved for treating dementia, we

Emerging evidence suggests adenosine G protein-coupled receptors (GPCRs) are promising therapeutic targets The adenosine A1 and A2A receptors are expressed in the human brain and have a proposed involvement in Targeting these receptors preclinically can mitigate pathogenic β-amyloid and tau neurotoxicity whilst accessible summary of the literature on Alzheimer's disease and the therapeutic potential of A1 and A2A receptors Although there are no available medicines targeting these receptors approved for treating dementia, we

protein-coupled receptor signaling kinetics and concentration-dependent responses using ONE-GO biosensors Computational Chemistry Postdoc in GPCR mechanosensing   Postdoctoral Position GPCR Activation and Signaling signaling suppresses feeding and weight gain in female rats Neuropeptide and serotonin co-transmission protein-coupled receptor-based autocrine screening for secondary metabolite production in yeast Protocol to investigate G protein-coupled receptor signaling kinetics and concentration-dependent responses using