Search Results

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. They have a common structure and, signaling through a much smaller set of G proteins, arrestins, and Phenotypic characterization suggests these mutations induce perturbation of G protein activation and/

September 2022 Endothelin-1 Stimulates PAI-1 Protein Expression via Dual Transactivation Pathway Dependent evaluate the role of dual transactivation of EGF and TGF-β receptors in phosphorylation of Smad2L and protein In addition, as an intermediary of G protein-coupled receptor (GPCR) signaling, the functions of ROCK Proteins were investigated<br />by western blotting using protein-specific antibodies against phospho-Smad2 This study is the first attempt to scrutinize the significant role of ROCK in the protein expression

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

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

Odorant G protein-coupled receptors as potential therapeutic targets for adult diffuse gliomas: a systematic analysis and review Odorant receptors (ORs) account for about 60% of all human G protein-coupled receptors

G protein-coupled receptor kinase 2 is essential to enable vasoconstrictor-mediated arterial smooth muscle production and circulation of vasoconstrictors, resulting in enhanced signalling through their cognate G protein-coupled GPCR signalling through phosphoinositide 3-kinase (PI3K)/protein kinase B (Akt) promotes VSMC proliferation In VSMC, G protein-coupled receptor kinase 2 (GRK2) is known to regulate numerous vasoconstrictor GPCRs

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.

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

October 2022 "We describe production of the human A2A adenosine receptor (A2AAR), a class A G protein-coupled

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

phosphorylation, β-arrestin binding and endocytosis, and a very high basal rate of degradation that is not protected

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

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

Calcium (Ca2+) signaling is known to direct processes that govern chondrocyte gene expression, protein that long-term CNO stimulatory culture have on hM3Dq [Ca2+]i signaling dynamics, proliferation, and protein This study demonstrated Gαq-G-protein coupled receptor (GPCR)-mediated [Ca2+]i signaling involvement

Genome-wide identification of 216 G protein-coupled receptor (GPCR) genes from the marine water flea Diaphanosoma celebensis G protein-coupled receptors (GPCRs) are considered to have originated from early

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

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

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

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

September 2022 "The bioactive lysophospholipid sphingosine-1-phosphate (S1P) acts via five different subtypes of S1P receptors (S1PRs) - S1P1-5. S1P5 is predominantly expressed in nervous and immune systems, regulating the egress of natural killer cells from lymph nodes and playing a role in immune and neurodegenerative disorders, as well as carcinogenesis. Several S1PR therapeutic drugs have been developed to treat these diseases; however, they lack receptor subtype selectivity, which leads to side effects. In this article, we describe a 2.2 Å resolution room temperature crystal structure of the human S1P5 receptor in complex with a selective inverse agonist determined by serial femtosecond crystallography (SFX) at the Pohang Accelerator Laboratory X-Ray Free Electron Laser (PAL-XFEL) and analyze its structure-activity relationship data. The structure demonstrates a unique ligand-binding mode, involving an allosteric sub-pocket, which clarifies the receptor subtype selectivity and provides a template for structure-based drug design. Together with previously published S1PR structures in complex with antagonists and agonists, our structure with S1P5-inverse agonist sheds light on the activation mechanism and reveals structural determinants of the inverse agonism in the S1PR family." Read more at the source #DrGPCR #GPCR #IndustryNews

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 "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

This emphasizes the importance of the Gi/o (pertussis toxin-sensitive G proteins, whose βγ subunits activate Our observations with these prominent commonalities may provide new insights into the phenotype and characteristics

Here, we sought to investigate the role of Regulator of G Protein Signaling 7 (RGS7) in hyperlipidemia-dependent

polystyrene nanoparticles in the range of μg/L in C. elegans The aim of this study was to identify Gα proteins mediating function of neuronal G protein-coupled receptors (GPCRs) in controlling the response to polystyrene an animal model, and both gene expression and functional analysis were performed to identify the Gα proteins Therefore, neuronal Gα proteins of GOA-1, GSA-1, and GPA-10 functioned to transduce signals of multiple