September 2022 "Yeast use the G-protein–coupled receptor signaling pathway to detect and track the mating The G-protein–coupled receptor pathway is inhibited by the regulator of G-protein signaling (RGS) Sst2 completion of cytokinesis before pheromone-induced polarity but is inhibited by unphosphorylated RGS binding

, Joshua Levitz for their work on Emerging modes of regulation of neuromodulatory G protein-coupled receptors GPCR Activation and Signaling Emerging modes of regulation of neuromodulatory G protein-coupled receptors adult male mice Methods & Updates in GPCR Research RNA therapeutics in targeting G protein-coupled receptors challenges Structural and Molecular Insights into GPCR Function Structural perspectives on chemokine receptors Pharmacology 2026 GPCR Jobs HIGHLIGHT Principal Scientist, In vitro pharmacology Senior Scientist - Receptor

the Process of Light-Induced Green Cone Pigment Activation Molecular dynamics-based identification of binding pathways and two distinct high-affinity sites for succinate in succinate receptor 1/GPR91 Specific pharmacological responses of some native GPCRs in neurons Beyond the Nucleus: Plastic Chemicals Activate G Protein-Coupled Receptors GPCRs in Neuroscience A M1 muscarinic acetylcholine receptor-specific positive allosteric modulator genomic analysis restricted to variants impacting gene function Interaction modes of human orexin 2 receptor

GPVI-Dependent Thrombus Formation under Shear "Glycoprotein (GP)VI and integrin αIIbβ3 are key signaling receptors integrin-dependent roles of focal adhesion kinase (protein tyrosine kinase 2, PTK2), the shear-dependent collagen receptor GPR56 (ADGRG1 gene), and calcium and integrin-binding protein 1 (CIB1). We designed and synthetized peptides that interfered with integrin αIIb binding (pCIB and pCIBm) or mimicked

Checkpoint for NK Cell Migration GPCR Activation and Signaling Subcellular activation of β-adrenergic receptors screening, molecular docking and dynamics simulation studies to identify potential agonists of orphan receptor ANN-QSAR models in the context of Alzheimer's disease GPCRs in Oncology and Immunology Aberrant hormone receptors regulate a wide spectrum of endocrine tumors G protein coupled receptor transcripts in human immune and their ligands in animal domestication The repertoire of G-protein-coupled receptor variations in

Matthew Belousoff et al. for their work on Lipid-Dependent Activation of the Orphan G Protein-Coupled Receptor Signaling Probing Activation and Conformational Dynamics of the Vesicle-Reconstituted β2 Adrenergic Receptor at the Single-Molecule Level Pharmacological characterization of seven human histamine H3 receptor isoforms Lipid-Dependent Activation of the Orphan G Protein-Coupled Receptor, GPR3 After wounding, a G-protein coupled receptor promotes the restoration of tension in epithelial cells GPCR Binders, Drugs, and more

Bioorthogonal Tethering Enhances Drug Fragment Affinity for G Protein-Coupled Receptors in Live Cells Differential Responses of the GLP-1 and GLP-2 Receptors to N-Terminal Modification of a Dual Agonist. Therapeutic antagonism of the neurokinin 1 receptor in endosomes provides sustained pain relief. Structural genomics of the human dopamine receptor system Structural Insights into Molecular Recognition and Receptor Activation in Chemokine–Chemokine Receptor Complexes Industry News Mavorixafor reduces

Inverse agonism of lysophospholipids with cationic head groups at Gi-coupled receptor GPR82. Asymmetric activation of dimeric GABAB and metabotropic glutamate receptors. Autocrine proteinase-activated receptor signaling in PC3 prostate cancer cells. Development, synthesis and evaluation of novel fluorescent Endothelin-B receptor probes. G protein-coupled receptors as targets for transformative neuropsychiatric therapeutics.

Significant advancements in the cellular biology of G protein-coupled receptors (GPCRs) about a novel biosensor shed light on the endosomal proteome associated with the δ-opioid receptor (DOR). The findings suggest that DNAJC13 is crucial to the trafficking of DOR, facilitating its downregulation In this study, the DOR receptor was genetically fused to APEX2, creating a DOR-APEX2 construct. the vicinity, allowing the capture of a snapshot of the endosomal proteome associated with the DOR receptor

GPCR Activation and Signaling A multi-dimensional view of context-dependent G protein-coupled receptor Molecular Modeling Study of a Receptor-Orthosteric Ligand-Allosteric Modulator Signaling Complex. GPCR Binders, Drugs, and more MRAP2 regulates energy homeostasis by promoting primary cilia localization distinct from the cannabinoid CB1 and CB2 receptors. Structural and Molecular Determinants for Isoform Bias at Human Histamine H3 Receptor Isoforms.

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.

homo- and heterodimers Structural basis of G protein-Coupled receptor CMKLR1 activation and signaling induced by a chemerin-derived agonist Functional profiling of the G protein-coupled receptor C3aR1 reveals conjugate ligands of the kappa-opioid receptor GPCRs in Neuroscience Research progress on the role of orphan receptor GPR139 in neuropsychiatric behaviours Rhodopsin orphan GPCR20 interacts with neuropeptides TRPA1 Expression Is Largely Limited to Sensory Neuron Subsets Orphan peptide and G protein-coupled receptor

ligands inhibit chemokine receptor heteromerization partners of α1B/D-adrenoceptors via interference Reviews, GPCRs, and more The leukotriene B4 receptors BLT1 and BLT2 as potential therapeutic targets. New paradigms in purinergic receptor ligand discovery. G protein-coupled receptor pharmacology - insights from mass spectrometry. Structural basis for motilin and erythromycin recognition by motilin receptor.

The targets, including G protein-coupled receptors (GPCRs), intracellular protein complexes and solute

in Adhesion GPCRs GPCR Activation and Signaling Diuretic hormone 31 activates two G protein-coupled receptors components of the Gαi3 heterotrimers Activation/Deactivation Free-Energy Profiles for the β2-Adrenergic Receptor , Drugs, and more Development of Photoswitchable Tethered Ligands that Target the µ-Opioid Receptor Design GPCRs in Neuroscience The Drosophila blood-brain barrier regulates sleep via Moody G protein-coupled receptor bioinformatics-based analysis Reviews, GPCRs, and more Parallel evolution of the G protein-coupled receptor

Kunitz-type snake toxin family associated with an original mode of interaction with the vasopressin 2 receptor from the Dendroaspis angusticeps venom is the most selective antagonist of the arginine-vasopressin V2 receptor MQs were produced by solid-phase peptide synthesis and characterized in vitro by binding and functional The number of MQ1 residues involved in V2R binding is large and may explain its absolute selectivity.

One potent form of inhibition is mediated by the activation of two inhibitory G protein-coupled receptors , D2 and GABAB receptors. Each of these receptors activates G protein-coupled inwardly rectifying potassium (GIRK) channels. The kinetics of the current induced by transient receptor activation is prolonged in each case. in the context of other G protein-coupled receptors."

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

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

approaches used in drug discovery create large datasets regarding ligand synthesis and screening, ligand binding sequences and molecular fingerprints coming from databases such as the GPCR-Ligand Association (GLASS), bindingDB docking and virtual screening can efficiently analyze large databases of compounds and predict their binding De novo drug design: AI algorithms can generate new molecules with desired properties, such as binding Predicting GPCR properties: AI models can predict various properties of GPCRs, such as ligand binding

coupling selectivity of GPCRs Location-biased activation of the proton-sensor GPR65 is uncoupled from receptor trafficking GPCR Binders, Drugs, and more An inverse agonist of orphan receptor GPR61 acts by a G protein-competitive Photoactivatable Agonist-Antagonist Pair as a Tool for Precise Spatiotemporal Control of Serotonin Receptor identification Reviews, GPCRs, and more The discovery, structure, and function of 5-HTR1E serotonin receptor drug discovery — but only if we give it the right data Inversago Pharma divulges new cannabinoid CB1 receptor

highlighted the most significant pathways associated with depression treatment, including neuroactive ligand-receptor molecular docking results showed that Polygalaxanthone III, Girinimbine and Pachymic acid performed greater binding HTR, DR, ADRA, AR, ESR, NR3C1) and modulate the activation of multiple pathways (Neuroactive ligand -receptor

effects on mouse metabolism Development, synthesis and evaluation of novel fluorescent Endothelin-B receptor endothelial activating GPR4 signals GPCRs in Neuroscience Involvement of a silkworm D2-like dopamine receptor Insights from Chronic Cholesterol Depletion Using Statin Side-Chain Dynamics of the α1B -Adrenergic Receptor determined by NMR via Methyl Relaxation Structural determinants of sphingosine-1-phosphate receptor selectivity Industry News Sosei Heptares and Verily Nominate First G-protein-coupled receptor Target

Hexahydroquinoline Derivatives are Selective Agonists for the Adhesion G Protein-Coupled Receptor ADGRG1 Autocrine Proteinase-Activated Receptor (PAR) signaling in PC3 prostate cancer cells. The G protein-coupled receptor neuropeptide receptor-15 modulates larval development via the transforming GPCR Binders, Drugs, and more Adenosine A2A Receptor (A2AAR) Ligand Screening Using the 19F-NMR Probe Stabilization of pre-existing neurotensin receptor conformational states by β-arrestin-1 and the biased

September 2022 " Background and purpose: The interaction of arrestins with G-protein coupled receptors (GPCRs) desensitizes agonist-dependent receptor responses and often leads to receptor internalization The interaction of arrestins with GPCRs requires both agonist activation and receptor phosphorylation the question whether agonists with very slow off-rates can cause the formation of particularly stable receptor-arrestin

GPCRs in Cardiology, Endocrinology, and Taste G-protein coupled receptor 19 (GPR19) knockout mice display GPCRs in Neuroscience GPR160 is not a receptor of anorexigenic cocaine- and amphetamine-regulated transcript Neurotensin receptor 1-biased ligand attenuates neurotensin-mediated excitation of ventral tegmental Methods & Updates in GPCR Research Activity Map and Transition Pathways of G Protein-Coupled Receptor Computational insights into ligand-induced G protein and β-arrestin signaling of the dopamine D1 receptor

24th, 2024 GPCR Activation and Signaling Calcium-Driven In Silico Inactivation of a Human Olfactory Receptor Deciphering the role of glycosaminoglycans in GPCR signaling G protein-coupled receptor-mediated autophagy prostatic hyperplasia GPCRs in Cardiology, Endocrinology, and Taste Blockade of endothelial adenosine receptor vivo through inhibiting CREB-ALK5-mediated endothelial to mesenchymal transition Role of pH-sensing receptors endogenous G proteins on endosomes and other organelles Reviews, GPCRs, and more G protein-coupled receptor

GPCRs in Cardiology, Endocrinology, and Taste G protein-coupled receptors driven intestinal glucagon-like Doxorubicin alters G-protein coupled receptor-mediated vasocontraction in rat coronary arteries GPCRs Using Protein Language Models Scaling up Functional Analyses of the G Protein-Coupled Receptor Rhodopsin Unraveling the Interplay of Extracellular Domain Conformational Changes and Parathyroid Hormone Type 1 Receptor Activation in Class B1 G Protein-Coupled Receptors: Integrating Enhanced Sampling Molecular Dynamics