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- Unlock the Future of GPCR Science: Breakthroughs and Courses Await | Sep 2 - Sep 8, 2024
Sirbu , Paolo Annibale , et al., for their study on Cell swelling enhances ligand-driven β-adrenergic signaling elegans The G protein-coupled receptor ADGRG6 maintains mouse growth plate homeostasis through IHH Signaling GPCR Activation and Signaling Illuminating GPCR trafficking Cell swelling enhances ligand-driven β-adrenergic signaling Roles of the gate loop in β-arrestin-1 conformational dynamics and phosphorylated receptor family members Structural basis of Frizzled 4 in recognition of Dishevelled 2 unveils mechanism of WNT signaling
- Network pharmacological investigation into the mechanism of Kaixinsan powder for the treatment of...
, including neuroactive ligand-receptor interaction pathway, serotonergic synapse pathway, PI3K-Akt signaling pathway and MAPK signaling pathway. indicated that the mechanism of KXS in treating depression was involved in the biological process of GPCR signal pathways (Neuroactive ligand -receptor interaction pathway, serotonergic synapse pathway, PI3K-Akt signaling pathway and MAPK signaling pathway)."
- 📰 GPCR Weekly News, March 18 to 24, 2024
GPCR Symposium on GPCR activation and signaling sessions. Let’s dive into the Classified GPCR News from March 18th to 24th, 2024 GPCR Activation and Signaling Silico Inactivation of a Human Olfactory Receptor Deciphering the role of glycosaminoglycans in GPCR signaling 2 - 7, 2024 | Chemotactic Cytokines June 9 - 14, 2024 | 2024 Phosphorylation and G-Protein Mediated Signaling
- Exciting GPCR Events for Next Year! + GPCR Weekly Rocket Launch ⦿ Oct 28 - Nov 3, 2024
/Structural Biologist Senior Scientist/Staff Scientist, Computational Chemistry GPCR Activation and Signaling GPCR signalling: Yet another variant route in a highly complex road map Transactivation of the EGF receptor study in Channa punctata GPCRs in Neuroscience Neuron specific quantitation of Gαolf expression and signaling in murine brain tissue Regulator of G protein signaling 6 (RGS6) in dopamine neurons promotes EtOH seeking of alcohol use disorders: Opportunities and hurdles for clinical development Chemokine CXCL13-CXCR5 signaling
- 📰 GPCR Weekly News, January 8 to 14, 2024
Adhesion GPCRs Conformational transitions and activation of the adhesion receptor CD97 GPCR Activation and Signaling Biased Signaling in Mutated Variants of β2-Adrenergic Receptor: Insights from Molecular Dynamics Simulations Propionate functions as a feeding-state-dependent regulatory metabolite to counter pro-inflammatory signaling diseases The progress of small molecules against cannabinoid 2 receptor (CB2R) Ketone bodies as chemical signals 2 - 7, 2024 | Chemotactic Cytokines June 9 - 14, 2024 | 2024 Phosphorylation and G-Protein Mediated Signaling
- Luciferase-based GloSensor™ cAMP assay: Temperature optimization and application to cell-based kinet
The second messenger cyclic adenosine monophosphate (cAMP) is a key mediator in many GPCR signaling pathways In this regard, luminescence-based biosensors have revolutionized our ability to monitor GPCR signaling The GloSensor™ cAMP assay enables real-time monitoring of signaling downstream of many GPCRs. As well, the GloSensor-22F biosensor had a superior signal-to-background ratio and the effect of temperature Nevertheless, the GloSensor™ cAMP assay can be applied to analyze signaling by a wide range of GPCRs
- 📰 GPCR Weekly News, June 26 to July 2, 2023
GPCR Activation and Signaling Trans-palmitoleic acid, a dairy fat biomarker, stimulates insulin secretion A unique melanocortin-4-receptor signaling profile for obesity-associated constitutively active variants GPCRs in Neuroscience Fine-tuning GPCR-mediated neuromodulation by biasing signaling through different GPCRs in Oncology and Immunology Dynamic Phosphoproteomics of BRS3 Activation Reveals the Hippo Signaling Autocrine proteinase-activated receptor signaling in PC3 prostate cancer cells.
- 📰 GPCR Weekly News, June 19 to 25, 2023
GPCR Activation and Signaling Stimulation of ectopically expressed muscarinic receptors induces IFN-γ mediated synaptic plasticity is independently regulated by location-specific receptor pools and divergent signaling GPCR Binders, Drugs, and more Molecular Characterization of Two Wamide Neuropeptide Signaling Systems PTK7 is a positive allosteric modulator of GPR133 signaling in glioblastoma. Antigen to New Therapeutics (June 30, 2023) FREE 11th Adrenoceptor Symposium: Adrenoceptors and GPCR Signalling
- 📰 GPCR Weekly News, May 8 to 14, 2023
GPCR Symposium on GPCR Activation and Signaling! GPCR Activation and Signaling Ligand-induced activation and G protein coupling of prostaglandin F2α receptor GPCRs in Cardiology, Endocrinology, and Taste Molecular Mechanisms of PTH/PTHrP Class B GPCR Signaling GPCRs in Oncology and Immunology DANGER Signals Activate G-Protein Receptor Kinases Suppressing Neutrophil Industry News InterAx Biotech to Apply its Leading AI and Cell Signalling Technology to Support Target
- Ode to GPCRs
The first Nobel prize that can be attributed to work related to GPCR-mediated signaling was the 1947 .[20,21] Adenylate cyclase is a major component of the downstream signaling cascade of the cAMP signal pathway, one of the two principal signal transduction pathways associated with GPCRs mediated signaling G protein-dependent signaling is the most well-known mechanism employed in GPCRs mediated signal transduction signaling pathways with other cellular signaling pathways, as well as non-signaling roles of GPCRs,
- What If Your Data is Lying to You? The Calcium Assay Dilemma
You’ll learn why calcium signals are inherently transient—giving rise to a “hemi-equilibrium” window
- Phosphorylation of RGS regulates MAP kinase localization and promotes completion of cytokinesis
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 which induces Gα GTPase activity and inactivation of downstream signaling. G-protein signaling activates the MAPK Fus3, which phosphorylates the RGS; however, the role of this
- 📰 GPCR Weekly News, November 13 to 19, 2023
Adhesion GPCRs CryoEM structures of adhesion in GPCR CD97: Filling in some of the gaps GPCR Activation and Signaling Butyrate induces STAT3/HIF-1α/IL-22 signaling via GPCR and HDAC3 inhibition to activate autophagy in Endosomal signaling via cAMP in parathyroid hormone (PTH) type 1 receptor biology β-arrestin1 is an E3 Nematode Species: Bursaphelenchus xylophilus and B. mucronatus GPCRs in Oncology and Immunology GPCR signaling contributes to immune characteristics of microenvironment and process of EBV-induced lymphomagenesis GPR56 signaling
- 📰 GPCR Weekly News, January 22 to 28, 2024
GPCR Symposia Our first upcoming symposium on March 15th this year is about GPCR activation and signaling Let’s dive into the Classified GPCR News from January 22nd to 28th, 2024 GPCR Activation and Signaling interactome analysis of α-arrestin families in human and Drosophila Functional diversification of cell signaling Associated Compounds in Cardiovascular Health and its Therapeutic Implications The perspective of cAMP/cGMP signaling 2 - 7, 2024 | Chemotactic Cytokines June 9 - 14, 2024 | 2024 Phosphorylation and G-Protein Mediated Signaling
- Single-molecule counting applied to the study of GPCR oligomerization
Consider G-protein-coupled receptors-an expansive class of transmembrane signaling proteins that participate While early evidence for the role of oligomerization in receptor signaling came from ensemble biochemical techniques to advance our understanding of the role of oligomerization in G-protein-coupled receptor signaling
- 📰 GPCR Weekly News, July 10 to 16, 2023
GPCR Activation and Signaling Bias comes in layers. GPCRs in Neuroscience The head mesodermal cell couples FMRFamide neuropeptide signaling with rhythmic Efferocytes release extracellular vesicles to resolve inflammation and tissue injury via prosaposin-GPR37 signaling GPCRs, and more Optical approaches for investigating neuromodulation and G Protein-Coupled Receptor signaling
- 📰 GPCR Weekly News, April 24 to 30, 2023
GPCR Symposium on GPCR Activation and Signaling on May 19th, 2023. Tethered agonist activated ADGRF1 structure and signalling analysis reveal basis for G protein coupling GPCR Activation and Signaling The ancestral ESCRT protein TOM1L2 selects ubiquitinated cargoes for retrieval A visual opsin from jellyfish enables precise temporal control of G protein signalling. Small-molecule targeting of GPCR-independent noncanonical G-protein signaling in cancer.
- 📰 GPCR Weekly News - January 2 to 8, 2023
GPCR Activation and Signaling Signal Transduction and Gene Regulation in the Endothelium. GPCR Signaling Measurement and Drug Profiling with an Automated Live-Cell Microscopy System. GPCRs in Oncology and Immunology Vasoactive intestinal peptide receptor 2 signaling promotes breast cancer STALICLA signs agreement with Novartis on neurodevelopmental disorders Call for GPCR Papers GPCRs: Signal
- Community guidelines for GPCR ligand bias: IUPHAR review 32
This 'biased signalling' paradigm requires that we now characterize physiological signalling not just Ligands eliciting biased signalling may constitute better drugs with higher efficacy and fewer adverse
- Dr. GPCR Updates
Read the podcast article GPCR Publication Highlights βCGRP breaks the mold: Distinct signaling patterns
- 📰 GPCR Weekly News, February 19 to 25, 2024
In just two weeks, on March 15th, we are hosting a symposium on GPCR activation and signaling. FMI-1) alters body size and regulates the composition of the extracellular matrix GPCR Activation and Signaling TIPE proteins control directed migration of human T cells by directing GPCR and lipid second messenger signaling ) in Himachal Pradesh, India Structural and Molecular Insights into GPCR Function Exploring Diverse Signaling 2 - 7, 2024 | Chemotactic Cytokines June 9 - 14, 2024 | 2024 Phosphorylation and G-Protein Mediated Signaling
- 📰 GPCR Weekly News, December 11 to 17, 2023
GPCR Activation and Signaling GPCR screening reveals that the metabolite receptor HCAR3 regulates epithelial of Gαq-PLCβ Interactions Snapshot of the cannabinoid receptor 1-arrestin complex unravels the biased signaling mechanism GPCR Binders, Drugs, and more Semi-synthetic nanobody-ligand conjugates exhibit tunable signaling rostral periventricular hypothalamic regions in female mice Cardiac optogenetics: shining light on signaling 2 - 7, 2024 | Chemotactic Cytokines June 9 - 14, 2024 | 2024 Phosphorylation and G-Protein Mediated Signaling
- Endogenous ligand recognition and structural transition of a human PTH receptor
PTHrP) bind to the parathyroid hormone receptor 1 (PTH1R) and activate the stimulatory G-protein (Gs) signaling Intriguingly, the two ligands have distinct signaling and physiological properties: PTH evokes prolonged complex process of ligand dissociation from the receptor and shed light on the distinct durations of signaling
- 📰 GPCR Weekly News, March 13 to 19, 2023
GPCR Activation and Signaling Components of TOR and MAP kinase signaling control chemotropism and pathogenicity A Rab10-ACAP1-Arf6 GTPases cascade modulates M4 muscarinic acetylcholine receptor trafficking and signaling Monitoring the Reversibility of GPCR Signaling by Combining Photochromic Ligands with Label-free Impedance proprietary chemo-informatics for GPCR drug discovery - Design Pharmaceuticals Call for GPCR Papers GPCRs: Signal (June 28 - 30, 2023) 11th Adrenoceptor Symposium: Adrenoceptors and GPCR Signalling (June 30 - July 1
- Exploiting Dependence of Castration-Resistant Prostate Cancer on the Arginine Vasopressin ...
September 2022 Exploiting Dependence of Castration-Resistant Prostate Cancer on the Arginine Vasopressin Signaling with a selective agonist desmopressin promoted CRPC cell proliferation through cAMP/protein kinase A signaling knockout of AVP in CRPC cells significantly reduced proliferation suggesting possible AVP autocrine signaling These data indicate that the AVP/arginine vasopressin receptor signaling axis represents a promising
- Unlocking the Therapeutic Potential of Previously Undruggable GPCRs
In general, signaling occurs when agonists engage key microswitch structures located in the TM domain , biased agonists that preferentially activate either G protein signaling or arrestin signaling, and superagonists with signaling activity higher than that of the native ligand (Figure 3). Figure 5: In an in vitro functional signaling assay on a human monocytic cell line, OB-004 demonstrated molecules for indications where subtle tuning of receptor signaling is required, or as vehicles for
- 📰 GPCR Weekly News, March 11 to 17, 2024
GPCR Symposium on GPCR activation and signaling a resounding success! Adhesion GPCRs ADGRG1, an adhesion G protein-coupled receptor, forms oligomers GPCR Activation and Signaling Diet-induced Mouse Model of Obesity GPCRs in Neuroscience Xanthurenic acid: A role in brain intercellular signaling 2 - 7, 2024 | Chemotactic Cytokines June 9 - 14, 2024 | 2024 Phosphorylation and G-Protein Mediated Signaling
- Glucagon receptor-mediated regulation of gluconeogenic gene transcription is endocytosis-dependent..
of G protein-coupled receptors (GPCRs) are now thought to use endocytosis to promote cellular cAMP signaling glucagon receptor (GCGR), which mediates physiological regulation of hepatic glucose metabolism via cAMP signaling Together, these results implicate the endosomal signaling paradigm in metabolic regulation by glucagon
- Endogenous ligand recognition and structural transition of a human PTH receptor
PTHrP) bind to the parathyroid hormone receptor 1 (PTH1R) and activate the stimulatory G-protein (Gs) signaling Intriguingly, the two ligands have distinct signaling and physiological properties: PTH evokes prolonged complex process of ligand dissociation from the receptor and shed light on the distinct durations of signaling
- Antibodies That Don’t Block, They Activate: A New Angle on Autoimmunity and GPCRs
“Some of these antibodies actually activate the receptor and cause pathological signaling.” — Tom Sakmar






