sympatholytic treatments (such as β-blockers) and renin-angiotensin system inhibitors or mineralocorticoid receptor Synthesis and release of these hormones in the adrenals is tightly regulated by adrenal G protein-coupled receptors (GPCRs), such as adrenergic receptors and AngII receptors. context of chronic HF, by focusing on the 2 best studied adrenal GPCR types in that context, adrenergic receptors and AngII receptors (AT 1 Rs).

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 modulation by Gβγ, but one - a GABAB receptor inhibits Ca2+ entry while another - a 5-HT1B receptor GABAB receptors alter Pr leaving synaptic properties unchanged, while 5-HT1B receptors fundamentally Co-activation of these receptors allows synaptic integration because of convergence of GABAB receptor

September 2022 "The glucagon-like peptide-1 receptor (GLP-1R) plays a key role in metabolism and is an

The sixth transmembrane region of a pheromone G-protein coupled receptor, Map3, is implicated in discrimination 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. Next, we swapped individual domains of Mam2 and Map3 with the respective domains in SoMam2 and SoMap3 , which revealed differences between the receptors both in the intracellular regions that regulate the

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

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.

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

neurotrophic factor-α1 (NF-α1/carboxypeptidase E, CPE) and human 5-HTR1E, a G protein-coupled serotonin receptor Thus, NF-α1/CPE uniquely interacts with serotonin receptor 5-HTR1E to activate the β-arrestin/ERK/CREB

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

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 (

) 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.

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

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

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

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

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

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 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

The mouse cytomegalovirus G protein-coupled receptor homolog, M33, coordinates key features of in vivo 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

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

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). addition, our results suggest a previously unknown sodium-binding site located in the extracellular domain of the CB1 receptor.

Phenylalanine 193 in Extracellular Loop 2 of the β 2-Adrenergic Receptor Coordinates β -Arrestin Interaction These receptors are the most clinically productive drug targets at present. components of receptor-effector interactions remain incompletely described. The β 2-adrenergic receptor ( β 2AR) is a prototypical and extensively studied GPCR that can provide SIGNIFICANCE STATEMENT: The role of extracellular G protein-coupled receptor (GPCR) domains in mediating

Dopamine receptors are involved in the modulation of fundamental physiological functions, and dysregulation We demonstrate that azodopa activates D1-like receptors in vitro in a light-dependent manner. Azodopa is the first photoswitchable dopamine agonist with demonstrated efficacy in wild-type animals

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

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

on the mechanism of signal activation, ligand selectivity and allosteric modulation in angiotensin receptors Thus, we need to know much more about the structures of receptor-ligand complexes at high resolution. Recently, X-ray structures of both AngII receptors (AT1 and AT2 receptors) bound to peptide and non-peptide , as the basis of ligand selectivity, efficacy, and regulation of the molecular functions of the receptors This review covers the new data elucidating the structural dynamics of AngII receptors and how structural

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