October 2022 "The role of different G protein-coupled receptors (GPCRs) in the cardiovascular system

We investigated the influence of specific inhibitors of G protein-coupled receptors (GPCR), endocytosis We performed a siRNA knockdown (KD) to assess the effect of Sigma-2 receptor (S2R) /Transmembrane Protein 97 (TMEM97)—a recently identified target protein of Hst1.

this review, we will discuss the regulation of mTORC1 by upstream stimuli, with a specific focus on G-protein

Synthesis and release of these hormones in the adrenals is tightly regulated by adrenal G protein-coupled a half that highlight the emerging roles of the GPCR-kinases and the β-arrestins in the adrenals, 2 protein

The sixth transmembrane region of a pheromone G-protein coupled receptor, Map3, is implicated in discrimination type depends on the molecular recognition of two peptidyl mating pheromones by their corresponding G-protein

Previously, we identified potent positive crosstalk between insulin/IGF-1 receptors and G protein-coupled

a Distinct Multi-Tiered Regulatory Network in the Intestinal Epithelium That Directs P-Glycoprotein Expression intestinal epithelium playing a pivotal role in removal of toxins and efflux of endocannabinoids to prevent excessive secondary bile acids, produced by the intestinal microbiome, potentiate the induction of functional P-gp expression sophisticated signaling network directed by intestinal microbial metabolites that orchestrate P-gp expression

SIGNIFICANCE STATEMENT Two G protein coupled receptors colocalize at presynaptic sites, to mediate presynaptic

G protein-coupled receptor kinase 2 is essential to enable vasoconstrictor-mediated arterial smooth muscle Using two indices of cell growth, we show that PI3K inhibition and depletion of GRK2 expression produced Moreover, GRK2 knockdown prevented endothelin-1 and angiotensin-II from increasing cyclin D1 expression These data suggest GRK2 expression is essential to facilitate vasoconstrictor-driven VSMC proliferation Considering VSMC GRK2 expression increases early in the development of hypertension, this highlights

Bitter taste receptors (TAS2Rs) are a poorly understood subgroup of G protein-coupled receptors (GPCRs

October 2022 "G protein-coupled receptors (GPCRs) are important drug targets characterized by a canonical

The mouse cytomegalovirus G protein-coupled receptor homolog, M33, coordinates key features of in vivo signalling repertoire Common to all cytomegalovirus (CMV) genomes analysed to date is the presence of G protein-coupled Constitutive G protein-coupled M33 signalling is required for these phenotypes, although the contribution constitutively activate phospholipase C β (PLCβ) and downstream cyclic AMP response-element binding protein IMPORTANCE G protein-coupled receptors (GPCRs) act as cell surface molecular "switches" which regulate

Role of G Protein-Coupled Receptors in Hepatic Stellate Cells and Approaches to Anti-Fibrotic Treatment G protein-coupled receptors (GPCRs) are cell surface receptors that mediate the function of a great variety It is predicted that more than 50 GPCRs are expressed in the liver. In this review, we describe the functions of multiple GPCRs expressed in HSCs, their roles in liver fibrogenesis

Odorant G protein-coupled receptors as potential therapeutic targets for adult diffuse gliomas: a systematic OR expression outside of the nose has functions distinct from odor perception, and may contribute to Here, we outlined the expression of brain ORs and investigated OR expression levels in glioma. Although most ORs were not ubiquitously expressed in gliomas, a subset of ORs displayed glioma subtype-specific expression.

August 2022 G protein-coupled receptor kinase type 2 and β-arrestin2: Key players in immune cell functions and inflammation "G protein-coupled receptor kinase type 2 (GRK2) and β-arrestin2 are representative proteins that regulate the transduction and trafficking of G protein-coupled receptor (GPCR) signaling The kinase GRK2 and the multifunctional scaffolding protein β-arrestin2 are key integrated signaling

diverse responses based on cell-specific G protein expression. Nevertheless, the diverse functionalities of various GPCRs, coupled with the fluctuating expression of , protein expression levels play a crucial role in determining the formation of protein complexes and Fine-tuned systems of protein expression regulate various processes, and their imbalance is linked to By comparing β-arrestin expression data in healthy tissues from the Genotype-Tissue Expression (GTEx)

October 2022 Coincident Regulation of PLCβ Signaling by Gq-Coupled and μOpioid Receptors Opposes Opioid- Mediated Antinociception "Pain management is a significant problem worldwide. The current frontline approach for pain-management is the use of opioid analgesics. The primary analgesic target of opioids is the μ-opioid receptor (MOR). Deletion of phospholipase Cβ3 (PLCβ3), or selective inhibition of Gβγ regulation of PLCβ3, enhances the potency of the antinociceptive effects of morphine suggesting a novel strategy for achieving opioid sparing effects. Here we investigated a potential mechanism for regulation of PLC signaling downstream of MOR in HEK293 cells and found that MOR alone could not stimulate PLC, but rather required a coincident signal from a Gq coupled receptor. Knockout of PLCβ3, or pharmacological inhibition of its upstream regulators, Gβγ or Gq, ex vivo in periaqueductal gray (PAG) slices increased the potency of the selective MOR agonist DAMGO in inhibiting presynaptic GABA release. Finally, inhibition of Gq-GPCR coupling in mice enhanced the antinociceptive effects of morphine. These data support a model where Gq and Gβγ-dependent signaling cooperatively regulate PLC activation to decrease MOR-dependent antinociceptive potency. Ultimately this could lead to identification of new non-MOR targets that would allow for lower dose utilization of opioid analgesics. " Read more at the source #DrGPCR #GPCR #IndustryNews Subscribe to the Newsletter HERE

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 Several members of MRGPRs are also expressed in mast cells, macrophages, and in cardiovascular tissue By stimulating human MRGPRD-expressing HeLa cells with the agonist β-alanine, we observed a release of

September 2022 "Adhesion G protein-coupled receptors (aGPCRs) are cell-surface proteins with large extracellular

Mutations in G protein-coupled receptors (GPCRs) underlie numerous diseases. We previously demonstrated rescue of cell surface expression of luteinizing hormone receptor mutants Seventeen FSHR mutations described in patients with reproductive dysfunction were expressed in HEK 293T Cell surface expression was severely reduced to ≤18% of wild-type (WT) for 11, modestly reduced to 66% of certain mutant FSHRs with severely reduced cell surface expression.

counting techniques enable a precise determination of the intracellular abundance and stoichiometry of proteins Consider G-protein-coupled receptors-an expansive class of transmembrane signaling proteins that participate the potential for these techniques to advance our understanding of the role of oligomerization in G-protein-coupled

GPR183 by 7 α,25-Dihydroxycholesterol Induces Behavioral Hypersensitivity through Mitogen-Activated Protein Kinase and Nuclear Factor- κ B "Emerging evidence implicates the G-protein coupled receptor (GPCR) GPR183 harvested at the time of peak hypersensitivity implicate potential contributions of mitogen-activated protein dependent on MAPK and NF-κB signaling pathways and results in an increase in pro-inflammatory cytokine expression

August 2022 "Abstract Sigma receptor is a transmembrane non-GPCR protein expressed mainly in the endoplasmic S1R has been implicated in many neurological disorders such as anxiety, schizophrenia, and depression

August 2022 "Three classes of G-protein-coupled receptor (GPCR) partners - G proteins, GPCR kinases,

conformational consequences of the differential activity of cannabidiol with two endocannabinoid-activated G-protein-coupled modulate different receptors in the endocannabinoid system, some of which belong to the family of G-protein-coupled investigate the interacting determinants of CBD in two closely related endocannabinoid-activated GPCRs, the G-protein-coupled

November 2022 "Adhesion G-protein-coupled receptors (aGPCRs) play key roles in a diversity of physiologies A comparison of Gq, Gs, Gi, and G12 engagements with ADGRL3 reveals the key determinant of G-protein Taken together, our study lays the groundwork for understanding aGPCR activation and G-protein-coupling

October 2022 "Recently determined structures of class C G protein-coupled receptors (GPCRs) revealed

October 2022 "Over three decades of research have provided thorough insights into G protein-coupled 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