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

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) 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.

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

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

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 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

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 To probe the activation mechanism of the Delta opioid receptor by an agonist ADL5859 started from inactive conformation using molecular dynamic simulations "The δ-opioid receptor (DOR) is a critical While the receptor with the crystal ligand (i.e. antagonist naltrindole) maintained the inactive conformation in all three independent simulations, the receptor with ADL5859 was adopting toward the active conformation

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

2022 "Morphine, the most widely used analgesic, relieves severe pain by activating the μ-opioid receptor

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

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

Opioid receptors are G-protein-coupled receptors (GPCRs) part of cell signaling paths of direct interest low pH at tissue targeted by opioid drugs in pain management could impact drug binding to the opioid receptor , because opioid drugs typically have a protonated amino group that contributes to receptor binding, In this review, we discuss the relationship between structure, function, and dynamics of opioid receptors from the perspective of the usefulness of computational studies to evaluate protonation-coupled opioid-receptor

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

October 2022 Coincident Regulation of PLCβ Signaling by Gq-Coupled and μOpioid Receptors Opposes Opioid The primary analgesic target of opioids is the μ-opioid receptor (MOR). found that MOR alone could not stimulate PLC, but rather required a coincident signal from a Gq coupled 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

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

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.

October 2022 "Visual phototransduction is the most extensively studied G protein-coupled receptor (GPCR

Integration and Spatial Organization of Signaling by G Protein-Coupled Receptor Homo- and Heterodimer complex organisms, cell to cell communication occurs mostly through neurotransmitters and hormones, and receptors The G protein-coupled receptors (GPCRs) are the largest family of membrane receptors, with nearly 800 evidence that supports these conjectures, fostering new ideas about the physiological role played by receptor

September 2022 Cannabinoid type-2 receptors: An emerging target for regulating schizophrenia-relevant brain circuits "Although the cannabinoid type-2 receptor (CB2) is highly expressed in the immune system Recent anatomical studies, combined with electrophysiological studies, indicate that CB2 receptors are effects of CB2 receptor activation, make this receptor an intriguing target for treating schizophrenia , has greatly advanced our understanding of this receptor.

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.

September 2022 Sweet taste receptor agonists attenuate macrophage IL‐1β expression and eosinophilic inflammation were assessed using specific inhibitor, genetic knockdown or knockout, and overexpression of cognate receptors