The 5HT2C serotonin receptor, which undergoes 32 distinct RNA-editing events leading to 24 protein isoforms These 5HT2C isoforms display differences in constitutive activity, agonist/inverse agonist potencies,

September 2022 "The GPR15 receptor is a G protein-coupled receptor (GPCR), which is activated by an endogenous peptide GPR15L(25-81) and a C-terminal peptide fragment GPR15L(71-81). Moreover, whether the receptor can also couple to Gs , Gq/11 and G12/13 is unclear. Here, GPR15L(25-81) and GPR15L(71-81) are used as pharmacological tool compounds to delineate the GPR15 The potencies of both peptides toward each Gi/o subtype have been determined.

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

September 2022 Structure of the human galanin receptor 2 bound to galanin and Gq reveals the basis of Three G-protein coupled receptors (GPCRs) for galanin have been discovered, which is the focus of efforts To understand the basis of the ligand preferences of the receptors and to assist structure-based drug

October 2022 Keratinocyte-derived defensins activate neutrophil-specific receptors Mrgpra2a/b to prevent skin dysbiosis and bacterial infection "Healthy skin maintains a diverse microbiome and a potent immune that the epithelial-cell-derived antimicrobial peptides defensins activated orphan G-protein-coupled receptors

Alterations in the expression and/or activity of brain G-protein-coupled receptors (GPCRs) such as dopamine functional role of kurarinone, an abundant lavandulated flavonoid in Sophora flavescens , on dopamine receptor With appreciable D2LR and D4R agonism and D1R antagonism, kurarinone might be a potential compound that

In this sense, G protein-coupled receptors (GPCRs) may be a good option to try to prolong our life while

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 Colocalization of different actions of GPCRs provide synaptic integration within presynaptic terminals 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

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

2022 Signaling pathways activated by sea bass gonadotropin-inhibitory hormone peptides in COS-7 cells transfected with their cognate receptor "Results of previous studies provided evidence for the existence of a functional and the potential interactions with sea bass kisspeptin (Kiss) signaling. with their cognate receptor GnIHR. Notably, GnIH2 antagonized Kiss2-evoked CRE-luc activity in COS-7 cells expressing GnIHR and Kiss2 receptor

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 Inflammation and Fibrosis; Potential Implications for Idiopathic Pulmonary Fibrosis "Idiopathic pulmonary 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 However, in epithelial cells, OGR1 promotes epithelial to mesenchymal transition (EMT) and inflammation

neurotrophic factor-α1 (NF-α1/carboxypeptidase E, CPE) and human 5-HTR1E, a G protein-coupled serotonin receptor and 125I NF-α1/CPE-binding studies demonstrated saturable, high-affinity binding to 5-HTR1E in stably transfected Thus, NF-α1/CPE uniquely interacts with serotonin receptor 5-HTR1E to activate the β-arrestin/ERK/CREB

Notably, G-protein-coupled receptors (GPCRs), representing the biggest drug target, have been revealed The gravity of this regulation becomes even more apparent when we consider the potential consequences Biased receptor signaling in drug discovery. Pharmacological Reviews, 71(2), 267-315. ERK-dependent apoptosis as a potential therapeutic strategy for cancer. Cells, 10(10), 2509. M., & Lefkowitz, R. J. (2003).

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 (

Mitogen-Activated Protein Kinase and Nuclear Factor- κ B "Emerging evidence implicates the G-protein coupled receptor of dorsal-horn spinal cord (DH-SC) tissues harvested at the time of peak hypersensitivity implicate potential

) 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.

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

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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

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 Considering VSMC GRK2 expression increases early in the development of hypertension, this highlights the potential

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

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 In addition, we have validated the H3R biosensor in membrane preparations and found that observed potency

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

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). pave the way for understanding the CBD pharmacology at a molecular level and aid in harnessing its potential

G protein-coupled receptors (GPCRs) are critical myocardial signal transducers which regulate cardiac models of cardiac pathology, and most pharmacological therapeutics currently used in HF target these receptors