August 2022 "Opioid receptors (ORs) represent one of the most significant groups of G-protein coupled receptor (GPCR) drug targets and also act as prototypical models for GPCR function.

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 Here, we report that the Ovarian Cancer G-Protein Coupled Receptor1 (OGR1 or GPR68) has dual roles in

September 2022 A2B Adenosine Receptor Enhances Chemoresistance of Glioblastoma Stem-Like Cells under we show for the first time that MRP3 expression is induced under hypoxia through the A2B adenosine receptor Downregulation of the A2B receptor decreases MRP3 expression and chemosensibilizes GSCs treated with These data suggest that hypoxia-dependent activation of A2B adenosine receptor promotes survival of GSCs

GABAB receptors inhibit Ca2+ entry, whereas 5-HT1B receptors target SNARE complexes. We demonstrate in male and female rats that GABAB receptors receptors alter Pr, whereas 5-HT1B receptors GABAB receptors alter Pr leaving synaptic properties unchanged, while 5-HT1B receptors fundamentally change properties of synaptic transmission, modifying AMPA receptor but sparing NMDA receptor responses Co-activation of these receptors allows synaptic integration because of convergence of GABAB receptor

The sixth transmembrane region of a pheromone G-protein coupled receptor, Map3, is implicated in discrimination the molecular recognition of two peptidyl mating pheromones by their corresponding G-protein coupled receptors Although such pheromone/receptor systems are likely to function in both mate choice and prezygotic isolation , very few studies have focused on the stringency of pheromone receptors. GPCRs might reflect the significantly distinct stringency/flexibility of their respective pheromone/receptor

August 2022 "The atypical chemokine receptor 1 (ACKR1) was discovered on erythrocytes as the Duffy blood group antigen ( Cutbush et al., 1950 ), also called Duffy-antigen/receptor for chemokines, or DARC (

One such platform is the chemogenetic DREADD (designer receptor exclusively activated by designer drugs This study demonstrated Gαq-G-protein coupled receptor (GPCR)-mediated [Ca2+]i signaling involvement

Nanobody binding stabilizes G-protein-coupled receptors (GPCR) in a fully active state and modulates conformational changes induced by the binding of a nanobody (Nb80) on the active-like β2 adrenergic receptor proximity of transmembrane (TM) helices 5 and 7, and favors the fully active-like conformation of the receptor contrast to the conditions under which no intracellular binding partner is bound, in which case the receptor intracellular loop 2 and extracellular loop 2 are captured from the trajectories of various ligand-bound receptors

Mitogen-Activated Protein Kinase and Nuclear Factor- κ B "Emerging evidence implicates the G-protein coupled receptor

The mouse cytomegalovirus G protein-coupled receptor homolog, M33, coordinates key features of in vivo repertoire Common to all cytomegalovirus (CMV) genomes analysed to date is the presence of G protein-coupled receptors 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

Numerous physiological effects of melatonin are mediated via its specific G protein-coupled receptors (GPCRs) named the MT1 receptor, which couples to both Gq and Gi proteins, and the MT2 receptor, which We investigated whether melatonin receptors are expressed on airway smooth muscle; whether they regulate We detected the mRNA and protein expression of the melatonin MT2 but not the MT1 receptor in native human Activation of melatonin MT2 receptors with either pharmacological concentrations of melatonin (10-100

G protein-coupled receptor kinase 2 is essential to enable vasoconstrictor-mediated arterial smooth muscle circulation of vasoconstrictors, resulting in enhanced signalling through their cognate G protein-coupled receptors In VSMC, G protein-coupled receptor kinase 2 (GRK2) is known to regulate numerous vasoconstrictor GPCRs

by sea bass gonadotropin-inhibitory hormone peptides in COS-7 cells transfected with their cognate receptor significantly decreased forskolin-elicited CRE-luc activity in COS-7 cells transfected with their cognate receptor Notably, GnIH2 antagonized Kiss2-evoked CRE-luc activity in COS-7 cells expressing GnIHR and Kiss2 receptor

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 (Daphnia magna) reveals a high level of orthological relationship of amine, neuropeptide, and opsin receptor repertoire, while purinergic and chemokine receptors were highly differentiated in humans.

August 2022 A NanoBRET-Based H 3 R Conformational Biosensor to Study Real-Time H 3 Receptor Pharmacology Membranes and Living Cells "Conformational biosensors to monitor the activation state of G protein-coupled receptors addition to the molecular pharmacology assay toolbox to characterize ligand efficacy at the level of receptor We recently reported the initial characterization of a NanoBRET-based conformational histamine H3 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

Phenylalanine 193 in Extracellular Loop 2 of the β 2-Adrenergic Receptor Coordinates β-Arrestin Interaction G protein-coupled receptors (GPCRs) transduce a diverse variety of extracellular stimuli into intracellular These receptors are the most clinically productive drug targets at present. Despite decades of research on the signaling consequences of molecule-receptor interactions, conformational components of receptor-effector interactions remain incompletely described.

) that cause nephrogenic diabetes insipidus "Loss-of-function mutations of the arginine vasopressin receptor AVPR2 is a kind of G protein coupled receptor (GPCR) and mainly couples with Gαs protein leading to cAMP Investigation into the characterization of biased receptors may give insights into the relationship between 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.

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

proteomes, we identified lysosomal cholesterol signaling (LYCHOS, previously annotated as G protein-coupled receptor

consequences of the differential activity of cannabidiol with two endocannabinoid-activated G-protein-coupled receptors In particular, CBD is able to modulate different receptors in the endocannabinoid system, some of which belong to the family of G-protein-coupled receptors (GPCRs). 55 (GPR55) and the cannabinoid type 1 receptor (CB1). Prompted by these results, we investigated the role of the CBD compound on the CB1 receptor using similar

September 2022 Microbial Metabolites Orchestrate a Distinct Multi-Tiered Regulatory Network in the Intestinal Epithelium That Directs P-Glycoprotein Expression "P-glycoprotein (P-gp) is a key component of the intestinal epithelium playing a pivotal role in removal of toxins and efflux of endocannabinoids to prevent excessive inflammation and sustain homeostasis. Recent studies revealed butyrate and secondary bile acids, produced by the intestinal microbiome, potentiate the induction of functional P-gp expression. We now aim to determine the molecular mechanism by which this functional microbiome output regulates P-gp. RNA sequencing of intestinal epithelial cells responding to butyrate and secondary bile acids in combination discovered a unique transcriptional program involving multiple pathways that converge on P-gp induction. Using shRNA knockdown and CRISPR/Cas9 knockout cell lines, as well as mouse models, we confirmed the RNA sequencing findings and discovered a role for intestinal HNF4α in P-gp regulation. These findings shed light on a sophisticated signaling network directed by intestinal microbial metabolites that orchestrate P-gp expression and highlight unappreciated connections between multiple pathways linked to colonic health." Read more at the source #DrGPCR #GPCR #IndustryNews

September 2022 Isoforms of GPR35 have distinct extracellular N-termini that allosterically modify receptor-transducer coupling and mediate intracellular pathway bias "Within the intestine, the human G protein-coupled receptor activation and signaling of 10 different heterotrimeric G proteins, ligand-induced arrestin recruitment, and receptor results reveal that the extended N-terminus of the long isoform limits G protein activation yet elevates receptor-β-arrestin contributed by the extended N-terminus of the long GPR35 isoform limits the extent of agonist-induced receptor-β-arrestin2

, essential to maintaining proper cardiac output and circulation, is regulated by G protein-coupled receptor

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