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October 2022 Dimerization of β2-adrenergic receptor is responsible for the constitutive activity subjected Here, we revealed that dimerization of β2-AR is responsible for the constitutive activity of β2-AR generating

September 2022 "The endocannabinoid system plays a key role in the intersection of the nervous, endocrine, and immune systems, regulating not only their functions but also how they interplay with each other. Endogenous ligands, named endocannabinoids, are produced “on demand” to finely regulate the synthesis and secretion of hormones and neurotransmitters, as well as to regulate the production of cytokines and other proinflammatory mediators. It is well known that immune challenges, such as exposure to lipopolysaccharide, the main component of the Gram-negative bacteria cell wall, disrupt not only the hypothalamic–pituitary–adrenal axis but also affects other endocrine systems such as the hypothalamic–pituitary–gonadal axis and the release of oxytocin from the neurohypophysis. Here we explore which actors and molecular mechanisms are involved in these processes." Read more at the source #DrGPCR #GPCR #IndustryNews

In CD8 + T cells, the chemokines promote unique transcriptional responses predicted to regulate inflammatory Our work demonstrates that differential subcellular signaling is critical to the overall biased response

Here, we revealed that dimerization of β2-AR is responsible for the constitutive activity of β2-AR generating

September 2022 GASP1 enhances malignant phenotypes of breast cancer cells and decreases their response Besides, we found that GASP1 knockout obviously improved the response of breast cancer cells to paclitaxel demonstrates that GASP1 enhances malignant behaviors of breast cancer cells and decreases their cellular response

August 2022 "Oxysterols induce the migration of B-lymphocytes and dendritic cells to interfollicular regions of lymphoid tissues through binding the EBI2 (GPR183) to stimulate effective adaptive immunity and antibody production during infection. Aberrant EBI2 signaling is implicated in inflammatory bowel disease, sclerosis, and infectious disease. Here, we report the cryo-EM structures of an EBI2-Gi signaling complex with its endogenous agonist 7α,25-OHC and that of an inactive EBI2 bound to the inverse agonist GSK682753A. These structures reveal an agonist binding site for the oxysterol and a potential ligand entrance site exposed to the lipid bilayer. Mutations within the oxysterol binding site and the Gαi interface attenuate G protein signaling and abolish oxysterol-mediated cell migration indicating that G protein signaling directly involves in the oxysterol-EBI2 pathway. Together, these findings provide new insight into how EBI2 is activated by an oxysterol ligand and will facilitate the development of therapeutic approaches that target EBI2-linked diseases." Read more at the source #DrGPCR #GPCR #IndustryNews

September 2022 "The activation of phospholipase C (PLC) is thought to have a key role in the cardiomyocyte response

Neuronal Gα subunits required for the control of response to polystyrene nanoparticles in the range of identify Gα proteins mediating function of neuronal G protein-coupled receptors (GPCRs) in controlling the response for understanding the important function of GPCRs-Gα signaling cascade in the neurons in controlling response

August 2022 GRK2 selectively attenuates the neutrophil NADPH-oxidase response triggered by β-arrestin recruiting GPR84 agonists "In order to avoid a prolonged pro-inflammatory neutrophil response, signaling

Nuclear magnetic resonance (NMR) spectroscopy allows the determination of atomic-level information on

Immunology Molecular characterization of breast cancer cell pools with normal or reduced ability to respond to progesterone: a study based on RNA-seq Reviews, GPCRs, and more Tri-part NanoLuc as a new split technology

However, basic physiology of PFC astrocytes, including which neuromodulatory signals they respond to signaling signatures in mouse astrocytes of the PFC and primary sensory cortex, which show differential responsiveness We find that PFC astrocytes express receptors for dopamine but are unresponsive through the Gs/Gi-cAMP

We show that both cell lines express KISS1R mRNA and respond to KP-10 by elevating calcium mobilisation Moreover, only BT-20 cells responded to KP-10 by increasing ERK phosphorylation in a β-arrestin-dependent universally true that kisspeptin/KISS1R stimulate migration or pro-metastatic behaviour, as divergent responses

in monocytes and macrophages indicates their involvement in immune cell trafficking and inflammatory responses of a diverse array of GPCRs in immune cells underscores their potential roles in modulating immune responses receptors in monocytes and macrophages suggest that these GPCRs could be targeted to modulate inflammatory responses

the movement of leukocytes throughout the body, ensuring a functional immune system and an effective response either limit chemokines spatial availability or to remove them from in vivo sites, while maintaining the responsiveness Scavenging allows cells to continuously migrate by remaining responsive to chemokines, it dampens the inflammatory response when needed; and it may interfere with other chemokine receptors which share the

Part II: Cell Cycle, DNA Damage Response, and Apoptosis Pathways Spliceosome mutations are associated with clinical response in a phase 1b/2 study of the PLK1 inhibitor onvansertib in combination with decitabine arrive Form and Function - Consequences of subcellular cAMP signaling revealed AI Predicts How GPCRs Respond

September 2022 "T cells are master regulators of the immune response tuning, among others, B cells, macrophages compartmentalization orchestrated in dynamic platforms is an essential requirement for the proper and efficient response Here, we discuss mechanisms responsible for signalling amplification and compartmentalization in T cell

Many such biosensors are based on the principle of Förster resonance energy transfer (FRET), and we have with FRET-based biosensors, we were able to track GPCR-dependent signaling pathways over time, and in response neuronal populations, we can quantify intracellular signaling while simultaneously measuring behavioral responses After several weeks to allow biosensor expression, fiber photometry is used in order to record drug responses

However, the magnitude of the response to this molecule varies considerably across this spectrum of mutations binding and folding suggests underlying differences in stability constrains the magnitude of their response comprehensive experimental characterization of the proteostatic properties of retinopathy variants and their response

Recent evidence indicates that GPR15 may be associated with modulation of the chronic inflammatory response and synovial tissue samples from RA patients, as well as to perform a functional migration assay in response Migration assays were performed using PBMCs isolated from these individuals in response to the synthetic

contractility, whereas stimulation of Gq-coupled receptors modulates cellular survival and hypertrophic responses We also review the hierarchy of signaling events driving the fibrotic response and the communications

This dual role opens new possibilities for more complex and nuanced cellular responses. feedback mechanisms and spatial localisation within the cell, is a crucial determinant of cellular responses The choice of pathway can result in different cellular responses, underscoring the criticality of precise immunofluorescence staining, HTRF (homogeneous time-resolved fluorescence), and TR-FRET (time-resolved fluorescence resonance

including endosomes, the Golgi apparatus, and the nuclear membrane, leading to spatially biased signaling responses Showing that this spatially biased signaling through arrestins can influence transcriptional responses cellular processes, including phospholipase C epsilon (PLCε)-dependent signaling and transcriptional responses localized to the nuclear membrane have emerged as important regulators of gene transcription and cellular responses underlying spatial bias in GPCR signaling involve both temporal and spatial components, sustained signaling responses

efficacies, and transduce to heterotrimeric G-proteins to generate different degrees of physiological responses studies with mutations of β1-AR residues show effects on the cellular signaling from β1-AR to the cAMP response

enabling a more detailed understanding of how genetic variation within human populations affects drug response By evaluating a broad spectrum of mutations, DMS can help predict which patient subpopulations will respond

patients Multiple sclerosis (MS) is a specific type of chronic immune-mediated disease in which the immune responses receptor axes network have crucial and efficacious impacts on behavior of the MSCs, nonetheless, the exact responsibility MSCs to migrate and home into the CNS of MS patients via expression of various chemokine receptors in response

of a ligand on a receptor's structure and biophysical attributes, and consequently on the biological response ligands can be categorized into four distinct efficacy classes: 1) full agonists produce the maximal response agonists), inhibition of activation (e.g., antagonists), or produce an inversion of the functional response

The G protein-coupled receptor GPRC5C is a saccharide sensor with a novel "off" response. Mammalian type Opsin 5 preferentially activates G14 in Gq-type G proteins triggering intracellular calcium response