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October 2022 "The activity of dopamine neurons is dependent on both intrinsic properties and afferent interaction between G βγ subunits and GIRK channels determines both the amplitude and kinetics of GPCR-dependent

October 2022 High hedgehog signaling is transduced by a multikinase-dependent switch controlling the

September 2022 Exploiting Dependence of Castration-Resistant Prostate Cancer on the Arginine Vasopressin

ago, GPCR activity was shown to be regulated by membrane potential in vitro, but whether the voltage dependence Here we show that muscarinic GPCR mediated neuronal potentiation in vivo is voltage dependent. Together, this study identifies a physiological role for the voltage dependency of GPCRs by demonstrating crucial involvement of GPCR voltage dependence in neuronal plasticity and behavior. Thus, this study suggests that GPCR voltage dependency plays a role in many diverse neuronal functions

October 2022 Glucagon receptor-mediated regulation of gluconeogenic gene transcription is endocytosis-dependent to use endocytosis to promote cellular cAMP signaling that drives downstream transcription of cAMP-dependent We show that epitope-tagged GCGRs undergo clathrin- and dynamin-dependent endocytosis in HEK293 and Huh We verify endocytosis-dependent induction of PCK1 expression by endogenous GCGRs in primary hepatocytes

October 2022 Cholesterol-Dependent Dynamics of the Serotonin1A Receptor Utilizing Single Particle Tracking

October 2022 β-arrestin1 and 2 exhibit distinct phosphorylation-dependent conformations when coupling

September 2022 "G protein-coupled receptors (GPCRs) are signaling hubs in cell membranes that regulate a wide range of physiological processes and are popular drug targets. Serotonin1A receptors are important members of the GPCR family and are implicated in neuropsychiatric disorders. Cholesterol is a key constituent of higher eukaryotic membranes and is believed to contribute to the segregated distribution of membrane constituents into domains. To explore the role of cholesterol in lateral dynamics of GPCRs, we utilized single particle tracking (SPT) to monitor diffusion of serotonin1A receptors under acute and chronic cholesterol-depleted conditions. Our results show that the short-term diffusion coefficient of the receptor decreases upon cholesterol depletion, irrespective of the method of cholesterol depletion. Analysis of SPT trajectories revealed that relative populations of receptors undergoing various modes of diffusion change upon cholesterol depletion. Notably, in cholesterol-depleted cells, we observed an increase in the confined population of the receptor accompanied by a reduction in diffusion coefficient for chronic cholesterol depletion. These results are supported by our recent work and present observations that show polymerization of G-actin in response to chronic cholesterol depletion. Taken together, our results bring out the interdependence of cholesterol and actin cytoskeleton in regulating diffusion of GPCRs in membranes." Read more at the source #DrGPCR #GPCR #IndustryNews

pharmaceutical company pioneering allosteric modulation-based drug discovery and development, today reported its half-year

Latrophilin-1 drives neuron morphogenesis and shapes chemo- and mechanosensation-dependent behavior in

By combining fiber photometry with FRET-based biosensors, we were able to track GPCR-dependent signaling

September 2022 Roles of Focal Adhesion Kinase PTK2 and Integrin αIIbβ3 Signaling in Collagen- and GPVI-Dependent Formation under Shear "Glycoprotein (GP)VI and integrin αIIbβ3 are key signaling receptors in collagen-dependent Here, we focused on disclosing the 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 - and GPVI-dependent thrombus formation, which is modulated by GPR56 and exclusively at high shear.

A role for BET proteins in regulating basal, dopamine-induced and cAMP/PKA-dependent transcription in One candidate effector of PKA-dependent transcriptional regulation is the BET protein Brd4. findings identify the BET protein family, and Brd4 in particular, as novel regulators of basal and D1R-dependent

September 2022 Endothelin-1 Stimulates PAI-1 Protein Expression via Dual Transactivation Pathway Dependent

Tailorable half-life: Nanobodies can extend their half-life through PEGylation or fusion to serum albumin This allows for tailoring the half-life of nanobodies to increase their therapeutic window depending

disease therapy Primary cilia in skeletal development and disease Industry News Addex Reports 2023 Half Trial with Cancer Immunotherapy Drug HTL0039732 Exscientia Business Update for Second Quarter and First Half

Topline results from 40 subjects are expected in the second half of the calendar year."

started from inactive conformation using molecular dynamic simulations Kinetic insights into agonist-dependent From Indivior In Extended Substance Use Disorder Research Collaboration Addex Therapeutics To Release Half-Year hand Sosei Heptares Operational Highlights and Consolidated Results for the Second Quarter and First Half

Particular emphasis is given to findings from the past decade and a half that highlight the emerging

Historically, drug discovery efforts targeting GPCRs focused on G-protein-dependent signaling pathways players in activating extracellular signal-regulated kinases (ERK) pathways alongside the G-protein dependent small GTPases like RAS leads to the activation of the MAP kinase kinase kinases (MAPKKKs), such as RAF RAF then phosphorylates and activates the MAP kinase kinases (MAPKKs), MEK1 and MEK2, which in turn phosphorylate ERK-dependent apoptosis as a potential therapeutic strategy for cancer. Cells, 10(10), 2509.

MI was introduced to rats by permanent left anterior descending coronary artery (LAD) ligation. Under normal conditions, β-catenin is degraded in the cytoplasm by the active GSK3β-dependent degradation

the field will have to face in the next 10 years is deciphering the physiological relevance of splice-dependent a lot of firsts in this perspective: the first time in a LATAM country, the first organized by Afro-descendants PMID 38421639 Systematic assessment of the tethered agonist-dependent activities of all 33 aGPCRs in

News Nxera Pharma Operational Highlights and Consolidated Results for the Second Quarter and First Half

labeled receptors GPCR Binders, Drugs, and more Orthosteric ligand selectivity and allosteric probe dependence binding mode GPCRs in Cardiology, Endocrinology, and Taste An extracellular glucose sensor for substrate-dependent to Vertex for $48 million Merck KGgA collaborates with Exscientia plc in deal worth up to $674M 2023 Half-Year

Roughly half of the receptors in the superfamily are sensory GPCRs, involved in olfaction, taste, vision ), meaning that lengthy pharmacodynamic activity is attained in vivo, despite the short circulatory half-life Twice-daily treatment with mOB-004 dose-dependently suppressed monocyte infiltration into the peritoneum