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August 2022 "Background: Activation of signaling effectors by G-protein coupled receptors (GPCRs) depends

G protein-coupled receptors (GPCRs) are crucial receptors that regulate a wide range of physiological

Thus, we investigated the regulatory functions of its β-adrenergic-like octopamine receptor (PxOctβ3) open reading frame (ORF) of PxOctβ3 was phylogenetically analyzed, and the levels of expression of the receptor A series of octopamine receptor agonists and antagonists were tested against PxOctβ3. We showed that the receptor is a member of the Octβ3 protein family, and an analysis using quantitative Furthermore, the agonists naphazoline, clonidine, 2-phenethylamine, and amitraz activated the PxOctβ3 receptor

October 2022 "Understanding the activation of G protein-coupled receptors (GPCRs) is of paramount importance to the field of cardiovascular medicine due to the critical physiological roles of these receptors and Although many cardiovascular GPCRs have been extensively studied as model receptors for decades, new

Although some G-protein coupled receptors (GPCRs) were reported to play roles in osteoblast function, GPR110 belongs to adhesion GPCR and was the functional receptor of N-docosahexaenoyl ethanolamine (also Synaptamide suppressed osteoclastogenesis induced by receptor activator of nuclear factor-kappa B ligand

August 2022 "GPR21 is an orphan and constitutively active receptor belonging to the superfamily of G-Protein Coupled Receptors (GPCRs).

August 2022 "The cannabinoid CB1 receptor is the most abundant G protein coupled receptor (GPCR) in A variety of ligands for CB1 receptors have been developed as promising drug candidates for the treatment New high-resolution structures of CB1 receptor in different functional states have significantly improved In this review, we describe the structural determinants for modulation of CB1 receptors by different types of ligands, as well as the differences between CB1 and its homologous, the CB2 receptor.

Class B G protein-coupled receptors (GPCRs) are notoriously difficult to target by small molecules because Using the parathyroid hormone type 1 receptor (PTHR) as a prototypic class B GPCR target, and a combination Here we found a key mechanical site that modulates the collective dynamics of the receptor and used this

Unexpectedly, Class A G protein-coupled receptors (GPCRs), a large class of signaling proteins exemplified by the visual receptor rhodopsin and its apoprotein opsin, are constitutively active as scramblases

They recognize two types of G protein-coupled receptors (LPARs): LPA1-3 receptors and LPA4-6 receptors This article provides an extensive review on the current status of ligand development targeting LPA receptors

September 2022 "The G-protein-coupled bile acid receptor, Gpbar1 or TGR5, is characterized as a membrane receptor specifically activated by bile acids. cAMP), Ras homolog family member A (RhoA), exchange protein activated by cAMP (Epac), and transient receptor

GPCR Podcast: Visualizing GLP-1 & GIP Receptors in Islets and Brain Understanding incretin biology depends on more than ligand potency — it hinges on where receptors actually are, how they internalize, and how Hodson walks through how his team uses fluorescence tools and chemically engineered ligands to map receptor Why this matters Receptor distribution shapes incretin hormone drug effects across islets and neural Fluorescent ligand engineering clarifies receptor behavior that cell lines can’t reveal.

August 2022 "Despite the importance of members of the GPCR superfamily as targets of a broad range of effective medicines many GPCRs remain poorly characterised. GPR84 is an example. Expression of GPR84 is strongly up regulated in immune cells in a range of pro-inflammatory settings and clinical trials to treat idiopathic pulmonary fibrosis are currently ongoing using ligands with differing levels of selectivity and affinity as GPR84 antagonists. Although blockade of GPR84 may potentially prove effective also in diseases associated with inflammation of the lower gut there is emerging interest in defining if agonists of GPR84 might find utility in conditions in which regulation of metabolism or energy sensing is compromised. Here, we consider the physiological and pathological expression profile of GPR84 and, in the absence of direct structural information, recent developments and use of GPR84 pharmacological tool compounds to study its broader role and biology. " Read more at the source #DrGPCR #GPCR #IndustryNews

(β2-AR), μ-opioid receptor (MOR), free fatty acid receptor 2 (FFA2R), and glucose-dependent insulinotropic , and endosomal trafficking for the glucagon-like-peptide-1 receptor (GLP-1R), β2-adrenergic receptor (β2-AR), µ-opioid receptor (MOR), free fatty acid receptor 2 (FFA2R), and glucose-dependent insulinotropic Conformational specificity of opioid receptors is determined by subcellular location irrespective of Endosomal signaling of delta opioid receptors is an endogenous mechanism and therapeutic target for relief

October 2022 Intermolecular Interactions in G Protein-Coupled Receptor Allosteric Sites at the Membrane Quantum Chemical Calculations "Allosteric modulators are called promising candidates in G protein-coupled receptor (GPCR) drug development by displaying subtype selectivity and more specific receptor modulation. Among the allosteric sites known to date, cavities at the receptor-lipid interface represent an uncharacteristic In this work, we analyze interactions in the allosteric sites of the PAR2, C5aR1, and GCGR receptors

October 2022 "Recently determined structures of class C G protein-coupled receptors (GPCRs) revealed this work, molecular docking screens for allosteric modulators targeting the metabotropic glutamate receptor The mGlu5 receptor is activated by the main excitatory neurotransmitter of the nervous central system , L-glutamate, and mGlu5 receptor activity can be allosterically modulated by negative or positive allosteric The mGlu5 receptor is a promising target for the treatment of psychiatric and neurodegenerative diseases

October 2022 Mechanism of enhanced sensitivity of mutated β-adrenergic-like octopamine receptor to amitraz Previous assays verified that a typical G protein-coupled receptor, β-adrenergic-like octopamine receptor

August 2022 "Histamine exerts its physiological functions through its four receptor subtypes. In this work, we report the subcellular localization of histamine receptor 2 (H2R), a G protein-coupled receptor (GPCR), which is expressed in a wide variety of cell and tissue types.

August 2022 "G-protein-coupled receptors (GPCR) are present at the cell surface in different conformational Here, we investigated this issue in living cells for the CC chemokine receptor 5 (CCR5), a major receptor in inflammation and the principal entry co-receptor for Human Immunodeficiency Viruses type 1 (HIV-1 We used TIRF microscopy and a statistical method to track and classify the motion of different receptor These results suggest a link between receptor activation and immobilization.

September 2022 "The follicle-stimulating hormone receptor (FSHR) belongs to the glycoprotein hormone receptors, a subfamily of G-protein-coupled receptors (GPCRs). site and is linked to the transmembrane domain by the hinge region (HR), is characteristic for these receptors

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

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

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

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

October 2022 Cholesterol-Dependent Dynamics of the Serotonin1A Receptor Utilizing Single Particle Tracking : Analysis of Diffusion Modes "G protein-coupled receptors (GPCRs) are signaling hubs in cell membranes 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

"Pepducins are small-lipidated peptides designed from the intracellular loops of G protein-coupled receptors The effect of pepducins at their cognate receptors has been shown to vary between antagonist, partial This review will focus in particular on pepducins designed from protease-activated receptors, C-X-C motif chemokine receptors, formyl peptide receptors, and the β2-adrenergic receptor. We will discuss the historic context of pepducin development for each receptor, as well as the structural

Biosensors for monitoring G protein-coupled receptors (GPCRs), the most drugged class of proteins in briefly summarize a subset of this field with accelerating importance: transducer biosensors measuring receptor-coupling and selectivity, with an emphasis on sensors measuring receptor association and activation of heterotrimeric

August 2022 "As important drug targets, G protein-coupled receptors (GPCRs) play pivotal roles in a wide We revealed that AlphaFold2 could capture the overall backbone features of the receptors.

cellular membrane's composition, organization, and physical properties might impact ligand binding, receptor membrane β-arrestin. β-arrestin reaches the receptor via lateral. Plasma membrane preassociation drives β-arrestin coupling to receptors and activation. Classical and new roles of b-arrestins in the regulation of G-protein-coupled receptors. Nat. Rev. Molecular mechanism of b-arrestin-biased agonism at seven-transmembrane receptors. Annu. Rev.

In this review, we focus on recent advances in G-protein-coupled receptor (GPCR) targets. To date, the most promising targets are the chemokine, cannabinoid, and dopamine receptors, but future work should further examine the melanocortin receptor-4 (MC4R), adhesion, lysophosphatidic acid (LPA ) and smoothened (Smo) receptors to initiate new drug-screening strategies and targeted delivery of safe