September 2022 Endothelin-1 Stimulates PAI-1 Protein Expression via Dual Transactivation Pathway Dependent expression of PAI-1 induced by endothelin-1 (ET-1) in bovine aortic endothelial cells (BAECs). Moreover, ET-1-increased protein expression of PAI-1 was decreased in the presence of bosentan (ET receptor expression of PAI-1<br />via induced the transactivation pathways of EGFR and TGFR. This study is the first attempt to scrutinize the significant role of ROCK in the protein expression

October 2022 "We describe production of the human A2A adenosine receptor (A2AAR), a class A G protein-coupled We explain in detail steps shared between the two sample preparation strategies, including expression

Biosensors for monitoring G protein-coupled receptors (GPCRs), the most drugged class of proteins in Their applications have continually expanded our understanding of this important protein class.

differentiation of MECs by assessing changes in cellular viability, lipid accumulation, and gene and protein expression of major milk protein and lipid synthesizing markers. using the HC11 cells as a model. We hypothesized that THC and CBD will negatively impact the synthesis of milk proteins and lipids, as Relative to control, 10μM THC and 10μM CBD reduced mRNA levels of milk proteins (CSN2 and WAP) , lipid and glucose transport markers (GLUT 1 , HK2 , FASN , FABP4 , PLIN2 and LPL) , as well as whey acidic protein

October 2022 Design and validation of recombinant protein standards for quantitative Western blot analysis radioligand binding assays with antibody-antigen interaction-based approaches for quantitative analysis of G protein-coupled receptor (GPCR) levels requires the use of purified protein standards containing the antigen. Results: Here we generated highly soluble and stable recombinant protein constructs GST-CB1414-472 and standard and negative control, respectively, in quantitative Western blot analysis of CB1 receptor expression

October 2022 Mechanistic Understanding of the Palmitoylation of Go Protein in the Allosteric Regulation of Adhesion Receptor GPR97 "Adhesion G-protein-coupled receptors (aGPCRs)-a major family of GPCRs-play Although it has been established that the palmitoylation of the C-terminal Go protein is essential for overall conformation of GPR97 is preferred to be fully active when interacting with palmitoylated Go protein provides mechanistic insights into the regulation of aGPCRs via post-translational modifications of the Go protein

September 2022 Cell-Type-Specific Effects of the Ovarian Cancer G-Protein Coupled Receptor (OGR1) on Proton-sensing G-protein coupled receptors are activated by acidic environments, but their role in fibrosis We demonstrate that OGR1 protein expression is significantly reduced in lung tissue from patients with IPF and that TGF-β1 decreases OGR1 expression. Our results suggest that strategies to selectively target OGR1 expression may represent a novel therapeutic

cryogenic-electron microscopy (cryo-EM) is used extensively to determine structures of activated G protein-coupled receptors (GPCRs) in complex with G proteins or arrestins. However, applying it to GPCRs without signaling proteins remains challenging because most receptors lack In GPCR crystallography, inserting a fusion protein between transmembrane helices 5 and 6 is a highly Here, we address this shortcoming by exploring different fusion protein designs, which lead to structures

October 2022 "Heterotrimeric G proteins couple activated G protein-coupled receptors (GPCR) to intracellular

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

August 2022 "As important drug targets, G protein-coupled receptors (GPCRs) play pivotal roles in a wide Recently, AlphaFold2 has been developed to predict structure models of many functionally important proteins

Significant advancements in the cellular biology of G protein-coupled receptors (GPCRs) about a novel This study, published in Nature Chemical Biology, highlights the role of the chaperone protein DNAJC13 During this process, APEX2 can label proteins in the vicinity, allowing the capture of a snapshot of After the labeling reaction, the researchers purified and biotinylated proteins (those that have been this analysis provided insights into the molecular composition of the endosomal environment and the proteins

Most acquired genes are transmembrane proteins and cytokines, such as viral G protein-coupled receptors (vGPCRs), chemokines, and chemokine-binding proteins.

October 2022 Intermolecular Interactions in G Protein-Coupled Receptor Allosteric Sites at the Membrane Simulations and Quantum Chemical Calculations "Allosteric modulators are called promising candidates in G protein-coupled

October 2022 Dual loss of regulator of G protein signaling 2 and 5 exacerbates ventricular myocyte Cardiac contractility, essential to maintaining proper cardiac output and circulation, is regulated by G protein-coupled Previously, the absence of regulator of G protein signaling (RGS) 2 and 5, separately, was shown to cause G protein dysregulation, contributing to modest blood pressure elevation and exaggerated cardiac hypertrophic Whether RGS2 and 5 redundantly control G protein signaling to maintain cardiovascular homeostasis is

A role for BET proteins in regulating basal, dopamine-induced and cAMP/PKA-dependent transcription in One candidate effector of PKA-dependent transcriptional regulation is the BET protein Brd4. suppressed the expression of ~25% of D1R-upregulated genes, while also increasing the expression of dopamine-induced genes in striatal neurons, and that knockdown of Brd4 attenuates D1R-induced gene expression Finally, we report that JQ1 treatment downregulated expression of many GPCRs and also impaired ERK1/2

September 2022 "The GPR15 receptor is a G protein-coupled receptor (GPCR), which is activated by an endogenous GPR15L(71-81) are used as pharmacological tool compounds to delineate the GPR15 receptor-mediated Gα protein signalling using a G protein activation assay and second messenger assay conducted on living cells.

Obesity-induced changes in human islet G protein-coupled receptor expression: Implications for metabolic regulation G protein-coupled receptors (GPCRs) are a large family of cell surface receptors that are insulin, and islet function can be modified by ligands acting at the large number of GPCRs that islets express , but one that is altered under pathophysiological conditions and, in this review, we have compared expression We have also considered the likely outcomes on islet function that the altered GPCR expression status

October 2022 "Biased G protein-coupled receptor (GPCR) ligands, which preferentially activate G protein behavior, reduced fertility, and memory impairment, which are potentially associated with impaired G protein In contrast to Gpr3-deficient mice, G protein-biased GPR3 mice do not display elevated anxiety levels We further determined that G protein-biased signaling reduces soluble Aβ levels and leads to a decrease glial response that may limit amyloid plaque development in G protein-biased GPR3 AD mice.

Integration and Spatial Organization of Signaling by G Protein-Coupled Receptor Homo- and Heterodimer The G protein-coupled receptors (GPCRs) are the largest family of membrane receptors, with nearly 800 genes coding for these proteins.

G protein-coupled receptor interactions and modification of signalling involving the ghrelin receptor and memory, gastrointestinal motility, glucose/lipid metabolism, the cardiovascular system, neuronal protection In vitro and in vivo data suggest that GHSR1a heterodimerises with multiple G protein-coupled receptors , serotonin 2C, orexin, oxytocin and melanocortin 3 receptors (MCR3), as well as the MCR3 accessory protein

October 2022 "Visual phototransduction is the most extensively studied G protein-coupled receptor (GPCR published cryo-electron tomography (cryo-ET) data on the ROS with structural knowledge on individual proteins

September 2022 Biased GPCR signaling by the native parathyroid hormone-related protein 1 to 141 relative to its N-terminal fragment 1 to 36 "The parathyroid hormone (PTH)-related protein (PTHrP) is indispensable amino acids, our current understanding on how endogenous PTHrP transduces signals through its cognate G-protein together, our results contribute to a better understanding of the biased signaling process of a native protein

Regulator G protein Signaling (RGS) proteins are critical components of the intracellular signaling pathways complexity, some members of the RGS family are selective for certain GPCRs, as a proof RGS4 which is expressed RGS4 is expressed in various immune cells, including T cells and B cells, and has been shown to modulate RGS4 acts as a negative regulator of T cell activation, and its expression is upregulated in response Hepler, Cellular regulation of RGS proteins: modulators and integrators of G protein signaling.

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 Recent studies showed that some AVPR2 mutations could cause biased Gαq/11 protein coupling rather than In this study, R68W and V162A were analyzed to whether they show a bias to Gαs or Gαq/11 proteins. R68W showed bias to coupling with Gαq/11 protein rather than V162A and wild-type receptor.

October 2022 "G protein-coupled receptors (GPCRs) are of considerable interest due to their importance in the cardiovascular system of the three most important GPCR signaling effectors: heterotrimeric G proteins We will first summarize their prominent roles in GPCR pharmacology before transitioning into less well-explored

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 By using the Cancer Genome Atlas (TCGA) and Gene Expression Omnibus (GEO) data, our analysis revealed Our analysis further supports the putative function of RGS proteins, particularly RGS20, in cancer."

September 2022 "Metabotropic γ-aminobutyric acid receptor (GABABR), a class C G protein-coupled receptor Cryo-electron microscopy studies revealed a drastic conformational change upon activation and a unique G protein