October 2022 "Arrestins interact with G protein-coupled receptors (GPCRs) to stop G protein activation Here, we report the cryo-electron microscopy active structure of the wild-type arginine-vasopressin V2 receptor described GPCR-arrestin assemblies, associated with an original V2R/β-arrestin1 interface involving all receptor

September 2022 "The human sweet taste receptor is a heterodimeric receptor composed of two distinct G-protein-coupled receptors (GPCRs), TAS1R2 and TAS1R3. As expected, the ligand affinities of hTAS1R2-VFT were drastically reduced through the introduction of acid substitutions (D278A and E382A) known to abolish the response of the full-length TAS1R2/TAS1R3 receptor

October 2022 Glucagon receptor-mediated regulation of gluconeogenic gene transcription is endocytosis-dependent in primary hepatocytes "A number of G protein-coupled receptors (GPCRs) are now thought to use endocytosis We tested if this is true for the glucagon receptor (GCGR), which mediates physiological regulation of

Prior to this report we did not know how different serotonin receptor subtypes which share high sequence The binding pockets for serotonin were virtually identical between the receptor-Gs and receptor-Gi complexes The structural differences found between the receptor-Gs and receptor-Gi complexes evidenced that 5-HT4 is 7.5 residues shorter compared to 5-HT1/4 receptors that couple to Gi/o. Interestingly, in the case of promiscuous receptors they found that these receptors shared conserved

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

September 2022 Cell Surface Calcium-Sensing Receptor Heterodimers: Mutant Gene Dosage Affects Ca 2+ Sensing but Not G Protein Interaction "The calcium-sensing receptor is a homodimeric class C G protein-coupled receptor (GPCR) that senses extracellular Ca2+ (Ca2+o ) via a dimeric extracellular Venus flytrap (VFT severe hyperparathyroidism (NSHPT), receptor function was markedly impaired. We consider how receptor asymmetry may support the underlying mechanisms. © 2022 The Authors.

November 2022 "Dimerization of beta 2-adrenergic receptor (β2-AR) has been observed across various physiologies

November 2022 "Despite the growing number of G protein-coupled receptor (GPCR) structures, only 39 structures

August 2022 "Fluorescently labeled ligands are versatile molecular tools to study G protein-coupled receptors fluorescent ligands targeting the intracellular allosteric binding site (IABS) of the CC chemokine receptor ligand, enabling cell-free as well as cellular NanoBRET-based binding studies in a non-isotopic and high-throughput

HEK293 cells reveals that both conventional and novel protein kinase C isozymes are involved in mGlu5a receptor internalization "The internalization of G protein-coupled receptors (GPCRs) can be regulated by PKC. to investigate the contribution of PKC isozymes in the internalization of the metabotropic glutamate receptor Direct activation of PKC and mutation of rat mGlu5a Ser901, a PKC-dependent phosphorylation site in the receptor C-tail, both showed that PKC isozymes facilitate approximately 40% of the receptor internalization.

August 2022 A correlation study of adhesion G protein-coupled receptors as potential therapeutic targets in Uterine Corpus Endometrial cancer "Adhesion G protein-coupled receptors (adhesion GPCRs), as a member of the G protein-coupled receptors (GPCRs) superfamily, have gradually entered the field of vision of

September 2022 Computational study of the conformational ensemble of CX3C chemokine receptor 1 (CX3CR1 ) and its interactions with antagonist and agonist ligands "The CX3C chemokine receptor 1 (CX3CR1), a member of the class A of G Protein-Coupled Receptors (GPCR) superfamily, and its ligand fractalkine In this work we present the study of the CX3CR1 receptor employing extensive atomistic Molecular Dynamics We analyzed the receptor conformational changes and described interactions within its key regions and

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 orthosteric binding pocket and the extracellular loops of D1R, D2LR, and D4R, validating substantial binding affinities

September 2022 "G protein-coupled receptors (GPCRs) are signaling hubs in cell membranes that regulate Serotonin1A receptors are important members of the GPCR family and are implicated in neuropsychiatric Our results show that the short-term diffusion coefficient of the receptor decreases upon cholesterol Analysis of SPT trajectories revealed that relative populations of receptors undergoing various modes Notably, in cholesterol-depleted cells, we observed an increase in the confined population of the receptor

cryogenic-electron microscopy (cryo-EM) is used extensively to determine structures of activated G protein-coupled receptors However, applying it to GPCRs without signaling proteins remains challenging because most receptors lack exploring different fusion protein designs, which lead to structures of antagonist bound A2A adenosine receptor

meningitidis is a Gram-negative opportunistic pathogen that is responsible for causing human diseases with high identified 30 N-acyl amides with representative members serving as agonists of the G-protein coupled receptor

September 2022 PLC-IP3-ORAI pathway participates in the activation of the MRGPRB2 receptor in mouse peritoneal mast cells "A novel mast cell-specific G-protein-coupled receptor (GPCR), known as Mas-related G protein-coupled receptor-B2 (MRGPRB2), plays important roles in immune response.

October 2022 Focusing on the role of secretin/adhesion (Class B) G protein-coupled receptors in placental syndrome mainly characterized by hypertension and proteinuria, with a worldwide incidence of 3–8% and high Obesity, immunological diseases and endocrine metabolic diseases are high-risk factors for the development G protein-coupled receptors, the largest family of membrane proteins in eukaryotes and the largest drug Among them, the secretin/adhesion (Class B) G protein-coupled receptors are essential drug targets for

September 2022 Lack of Oestrogen Receptor Expression in Breast Cancer Cells Does Not Correlate with Kisspeptin Signalling and Migration "Kisspeptin is an anti-metastatic mediator in many cancer types, acting through its receptor been associated with increased invasion and MMP-9 expression, leading to the suggestion that hormone receptor veracity of this claim, we compared endogenous KISS1R signalling and physiological output in the hormone receptor-negative

August 2022 "G-protein-coupled receptors (GPCRs) receive signals from ligands with different efficacies We report the cryo-EM structures of β1-adrenergic receptor (β1-AR) in complex with Gs (GαsGβ1Gγ2) and

neurotrophic factor-α1 (NF-α1/carboxypeptidase E, CPE) and human 5-HTR1E, a G protein-coupled serotonin receptor interaction between NFα1/CPE and 5-HTR1E and 125I NF-α1/CPE-binding studies demonstrated saturable, high-affinity Thus, NF-α1/CPE uniquely interacts with serotonin receptor 5-HTR1E to activate the β-arrestin/ERK/CREB

The 5HT2C serotonin receptor, which undergoes 32 distinct RNA-editing events leading to 24 protein isoforms

September 2022 "The GPR15 receptor is a G protein-coupled receptor (GPCR), which is activated by an endogenous However, the activation profiles of the GPR15 receptor within Gi/o subtypes have not been examined. Moreover, whether the receptor can also couple to Gs , Gq/11 and G12/13 is unclear. The results show that the GPR15 receptor preferentially couples to Gi/o rather than other pathways in Within the Gi/o family, the GPR15 receptor activates all the subtypes (Gi1 , Gi2 , Gi3 , GoA , GoB and

Crystal structures suggest ligand access to the orthosteric binding site of MT1 and MT2 receptors through entry route for 2-iodomelatonin, a nonselective agonist with a slower dissociation rate from the MT2 receptor which revealed different trajectories passing through the gap between TM helices IV and V for both receptors The side-chain flexibility of Tyr5.38 was significantly different in the two receptor subtypes, as assessed is a way of connecting the orthosteric binding site and the membrane core for lipophilic melatonin 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 that the epithelial-cell-derived antimicrobial peptides defensins activated orphan G-protein-coupled receptors

August 2022 A NanoBRET-Based H 3 R Conformational Biosensor to Study Real-Time H 3 Receptor Pharmacology 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 biosensor in membrane preparations and found that observed potency values better correlated with binding affinity Hence, the H3R conformational biosensor in membranes might be a ready-to-use, high-throughput alternative

September 2022 "The glucagon-like peptide-1 receptor (GLP-1R) plays a key role in metabolism and is an Given the high induction of GLP-1R in human iTreg cells, we hypothesize that GLP-1R+ iTreg cells play