Event Spotlight Discovery on Target’s 19th Annual GPCR-Based Drug Discovery Targeting G Protein-Coupled Receptors This technique for studying cell receptors could have sweeping implications for drug development DeepCure GPCR Latrophilin-1 controls multiple processes in reproduction of C. elegans The G protein-coupled receptor β-adrenergic signaling Roles of the gate loop in β-arrestin-1 conformational dynamics and phosphorylated receptor DNAJC13 in DOR downregulation GPCRs in Cardiology, Endocrinology, and Taste Role of G protein coupled receptors

November 2022 "Some G protein-coupled receptor (GPCR) ligands act as "biased agonists" that preferentially contributes to the biased signaling generated by three endogenous ligands of the GPCR CXC chemokine receptor mouse model of contact hypersensitivity, β-arrestin-biased CXCR3-mediated inflammation is dependent on receptor overall biased response observed at CXCR3, which has important implications for drugs targeting chemokine receptors

October 2022 "Adhesion G protein-coupled receptors (aGPCRs) are keys of many physiological events and via an autoproteolysis process that removes the inhibitory GAIN domain on the extracellular side of receptor and releases a stalk peptide to bind and activate the transmembrane side of receptor. This is also where Gq/Gs bind the receptor through both hydrophobic and polar interaction, while Gi/G12 /G13 engage receptor mainly through hydrophobic interaction.

Depending on which ligand activates a receptor, it can engage different intracellular transducers. 'biased signalling' paradigm requires that we now characterize physiological signalling not just by receptors but by ligand-receptor pairs. The guidelines will aid consistency and clarity, as the basic receptor research and drug discovery communities

GPCR Activation and Signaling Stimulation of ectopically expressed muscarinic receptors induces IFN-γ Serotonin 5-HT7 receptor slows down the Gs protein: a single molecule perspective. Striatal mGlu5-mediated synaptic plasticity is independently regulated by location-specific receptor in vitro Characterization of BAY 2686013, an Allosteric Small Molecule Antagonist of the Human PAC1 Receptor GPCR Research A coiled-coil-based design strategy for the thermostabilization of G-protein-coupled receptors

Specifically, we explore the role of actin cytoskeleton in regulating the dynamics of the serotonin1A receptor , a crucial neurotransmitter G protein-coupled receptor (GPCR) that plays a major role in the generation For this, we analyzed the lateral dynamics of the serotonin1A receptor in cholesterol-depleted cells Our results indicate that lateral diffusion parameters of serotonin1A receptors in normal cells are consistent Interestingly, these parameters are altered in cholesterol-depleted cells and the receptor exhibits dynamic

Christopher Langmead and colleagues' work on the 5-HT2C receptor as a therapeutic target for substance response of Tribolium castaneum GPCR Activation and Signaling Biased allosteric activation of ketone body receptor GPCRs in Oncology and Immunology [1,2,4]Triazolo[1,5-c]pyrimidines as Tools to Investigate A3 Adenosine Receptors correlates with increased level of autoantibodies targeting vasoregulatory and autonomic nervous system receptors Bound to Gs Protein and Exendin-P5 Biased Agonist Molecular and structural insights into the 5-HT2C receptor

Agonist-to-Antagonist Conversion: Enabling the Design of Nucleoside Functional Switches for the A2A Adenosine Receptor "Modulators of the G protein-coupled A2A adenosine receptor (A2AAR) have been considered promising agents Structural analysis revealed that the introduced thiophene modification restricted receptor conformational This approach can expand the repertoire of adenosine receptor antagonists that can be designed based

GPCR Binders, Drugs, and more Autoantibodies targeting G protein-coupled receptors: An evolving history Novel Xanomeline-Containing Bitopic Ligands of Muscarinic Acetylcholine Receptors: Design, Synthesis Intermediate-state-trapped mutants pinpoint G protein-coupled receptor conformational allostery. Structural basis of peptide recognition and activation of endothelin receptors. PhD Studentship - Insight Into The Neuroprotective Function Of The Prostaglandin Receptor Ep2.

GPCR Activation and Signaling Constitutive activity of the dopamine (D5 ) receptor, highly expressed Cholesterol Biases the Conformational Landscape of the Chemokine Receptor CCR3: A MAS SSNMR-Filtered intermedin is a slow off-rate, long-acting endogenous agonist of the adrenomedullin2 G protein-coupled receptor GPCRs in Neuroscience GPCR interactions involving metabotropic glutamate receptors and their relevance G protein-coupled receptors in neurodegenerative diseases and psychiatric disorders.

We previously demonstrated that the G protein-coupled receptor (GPCR) arginine vasopressin receptor type1A AVPR1A is part of a family of GPCR's including arginine vasopressin receptor type 2 (AVPR2). found that castration-resistant cells produced AVP, the endogenous ligand for arginine vasopressin receptors These data indicate that the AVP/arginine vasopressin receptor signaling axis represents a promising

August 2022 "Chemokines, a subgroup of cytokines along with their receptors, are involved in various C-X-C motif chemokine receptor 4 (CXCR4), a G-protein-coupled receptor (GPCR), has one identified natural

Classified GPCR News from March 11th to 17th, 2024 Adhesion GPCRs ADGRG1, an adhesion G protein-coupled receptor forms oligomers GPCR Activation and Signaling Unraveling the crosstalk between renin-angiotensin system receptors Insights from Gαi3 research GPCRs in Cardiology, Endocrinology, and Taste The Prostaglandin E2 EP3 Receptor : A role in brain intercellular signaling Are there sex differences in oxytocin and vasopressin V1a receptors visualize and quantify the COPII concentration and anterograde transport of nascent G protein-coupled receptors

GPCRs in Cardiology, Endocrinology, and Taste Dietary compounds activate an insect gustatory receptor Elucidation of a dynamic interplay between a beta-2 adrenergic receptor, its agonist, and stimulatory Function and structure of bradykinin receptor 2 for drug discovery. Developing novel antifungals: lessons from G protein-coupled receptors. PhD Studentship - Insight Into The Neuroprotective Function Of The Prostaglandin Receptor Ep2.

GPCR Activation and Signaling How can we improve the measurement of receptor signaling bias? The relaxin receptor RXFP1 signals through a mechanism of autoinhibition. Regulation of the pro-inflammatory G protein-coupled receptor GPR84. GPCR Binders, Drugs, and more Development of a 5-HT7 receptor antibody for the rat: the good, the bad GPCRs in Neuroscience G protein coupled receptors as targets for transformative neuropsychiatric therapeutics

steered molecular dynamics in uncovering the dissociation kinetics of ligands targeting G-protein-coupled receptors absolute residence times of the antagonist ZMA241385 and agonist NECA that target the A2A adenosine receptor of the G-protein-coupled receptor (GPCR) protein family. thermodynamics of ligand binding in terms of ligand binding energies and the per-residue contribution of the receptor

critical components of the intracellular signaling pathways that mediate the effects of G protein-coupled receptors For example, μ opioid receptor (MOR) interacts with Gαi/o and Gαz subunits, which have a slow enzymatic ; enhancing the activity of the G protein that is coupled to the receptor and leading to a decrease in Traynor, Differential modulation of mu- and delta-opioid receptor agonists by endogenous RGS4 protein Zhuang, Y., et al., Structural insights into the human D1 and D2 dopamine receptor signaling complexes

GPCR Binders, Drugs, and more Inhibiting a promiscuous GPCR: iterative discovery of bitter taste receptor Sodium is a negative allosteric regulator of the ghrelin receptor. GPCRs in Cardiology, Endocrinology, and Taste Novel roles for G protein-coupled receptor kinases in cardiac GPCRs in Neuroscience G protein-coupled receptors (GPCRs) as Potential Therapeutics for Psychiatric Disorders Transcriptomic profiling of sex-specific olfactory neurons reveals subset-specific receptor expression

Revealing the tissue-level complexity of endogenous glucagon-like peptide-1 receptor expression and signaling The cannabinoid receptor 1 antagonist AM6545 stimulates the Akt-mTOR axis and in vivo muscle protein Reviews, GPCRs, and more Olfactory Receptors as an Emerging Chemical Sensing Scaffold. Structural and Molecular Insights into GPCR Function The role of G protein conformation in receptor-G Ligands selectively tune the local and global motions of neurotensin receptor 1 (NTS1).

GPCR Activation and Signaling Ligand-induced activation and G protein coupling of prostaglandin F2α receptor Plasma membrane preassociation drives β-arrestin coupling to receptors and activation. An allosteric modulator of the adenosine A1 receptor potentiates the antilipolytic effect in rat adipose Reviews, GPCRs, and more Recent Studies on Serotonin 5-HT2A Receptor Antagonists in Medicinal Chemistry Mechanism of Activation of the Visual Receptor Rhodopsin.

The Wnt pathway protein Dvl1 targets Somatostatin receptor 2 for lysosome-dependent degradation. Loss of biased signaling at a G protein-coupled receptor in overexpressed systems. GPCR Binders, Drugs, and more A snake toxin as a theranostic agent for the type 2 vasopressin receptor Small-Molecule Fluorescent Ligands for the CXCR4 Chemokine Receptor. GPCRs in Cardiology, Endocrinology, and Taste Green mamba peptide targets type-2 vasopressin receptor

the paraventricular nucleus of the hypothalamus, where it interacts with various G protein-coupled receptors , such as the prokineticin receptors, and regulates energy expenditure and appetite. Understanding the mechanism by which MRAP2 regulates G protein-coupled receptors helps in elucidating

Discovery and In Vivo Evaluation of ACT-660602: A Potent and Selective Antagonist of the Chemokine Receptor CXCR3 for Autoimmune Diseases "The chemokine receptor CXCR3 is a seven-transmembrane G-protein-coupled receptor (GPCR) involved in various pathologies, in particular autoimmune diseases.

Event Spotlight Discovery on Target’s 19th Annual GPCR-Based Drug Discovery Targeting G Protein-Coupled Receptors Nxera Pharma’s Partner Centessa Announces Positive Interim Phase 1 Clinical Data with its Novel Orexin Receptor Postdoctoral research position Adhesion GPCRs Loss of cardiomyocyte-specific Adhesion G Protein Coupled Receptor energy homeostasis Eiken syndrome with parathyroid hormone resistance due to a novel parathyroid hormone receptor sensory input across polysynaptic circuitries in mouse visual cortex by a single G protein-coupled receptor

Lipids Are an Integral Part of Transmembrane Allosteric Sites in GPCRs: A Case Study of Cannabinoid CB1 Receptor Bound to a Negative Allosteric Modulator, ORG27569, and Analogs "A growing number of G-protein-coupled receptor in the access and binding of ORG27569 and its analogs at the transmembrane site of cannabinoid CB1 receptor

in living cells "β-arrestins mediate regulatory processes for over 800 different G protein-coupled receptors finger-loop-region, we show that the two isoforms prefer to associate with the active parathyroid hormone 1 receptor Here, we show differences between conformational changes that are induced by P-R* or R* receptor states

Adhesion GPCRs Dual role of the adhesion G-protein coupled receptor ADRGE5/CD97 in glioblastoma invasion G protein-coupled receptor-mediated membrane targeting of PLCγ2 is essential for neutrophil chemotaxis Monoacylglycerol Lipase Protects the Presynaptic Cannabinoid 1 Receptor from Desensitization by Endocannabinoids Endocrinology, and Taste Insights on discovery, efficacy, safety and clinical applications of ghrelin receptor GPCRs in Oncology and Immunology Interplay between G protein-coupled receptors and nanotechnology.

GPCRs in Neuroscience Photopharmacological manipulation of amygdala metabotropic glutamate receptor mGlu4 in Oncology and Immunology Pan-cancer functional analysis of somatic mutations in G protein-coupled receptors Stability. iORbase: a database for the prediction of the structures and functions of insect olfactory receptors Sosei Heptares' Partner Pfizer Progresses its Oral GLP-1 Receptor Agonist PF-07081532 into Phase 2 Clinical Deadline February 12, 2023 Current Technologies To Understand G-Protein-Coupled Receptor Molecular Pharmacology