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Results found for "Stephen S G Ferguson"

  • Regulation of rod photoreceptor function by farnesylated G-protein γ-subunits

    September 2022 "Heterotrimeric G-protein transducin, Gt, is a key signal transducer and amplifier in The only other farnesylated G-protein γ-subunit, Gγ11 (Gng11), is expressed in multiple tissues but not

  • Disentangling bias between G q, GRK2, and arrestin3 recruitment to the M 3 muscarinic acetylcholine

    G protein-coupled receptors (GPCRs) transmit extracellular signals to the inside by activation of intracellular Here, we compared the efficacy of seven agonists to induce G protein, G protein-coupled receptor kinase However, the rank order of the agonists for G protein- and GRK2-M3R interaction was the same, suggesting that G protein and GRK2 binding to M3R requires similar receptor conformations, whereas requirements

  • A correlation study of adhesion G protein-coupled receptors as potential therapeutic targets in...

    August 2022 A correlation study of adhesion G protein-coupled receptors as potential therapeutic targets in Uterine Corpus Endometrial cancer "Adhesion G protein-coupled receptors (adhesion GPCRs), as a member of the G protein-coupled receptors (GPCRs) superfamily, have gradually entered the field of vision of

  • Structural insights into adhesion GPCR ADGRL3 activation and Gq, Gs, Gi, and G12 coupling

    November 2022 "Adhesion G-protein-coupled receptors (aGPCRs) play key roles in a diversity of physiologies A comparison of Gq, Gs, Gi, and G12 engagements with ADGRL3 reveals the key determinant of G-protein Taken together, our study lays the groundwork for understanding aGPCR activation and G-protein-coupling

  • Fusion protein strategies for cryo-EM study of G protein-coupled receptors

    particle cryogenic-electron microscopy (cryo-EM) is used extensively to determine structures of activated G protein-coupled receptors (GPCRs) in complex with G proteins or arrestins.

  • Targeted Activation of G-Protein Coupled Receptor-Mediated Ca 2+ Signaling Drives Enhanced Cartilage

    This study demonstrated Gαq-G-protein coupled receptor (GPCR)-mediated [Ca2+]i signaling involvement

  • Chemogenetic stimulation of the G i pathway in astrocytes suppresses neuroinflammation

    Engineered G protein-coupled receptors (GPCRs) are commonly used in chemogenetics as designer receptors

  • Focusing on the role of secretin/adhesion (Class B) G protein-coupled receptors in placental...

    October 2022 Focusing on the role of secretin/adhesion (Class B) G protein-coupled receptors in placental G protein-coupled receptors, the largest family of membrane proteins in eukaryotes and the largest drug Among them, the secretin/adhesion (Class B) G protein-coupled receptors are essential drug targets for Given the great value of the secretin/adhesion (Class B) G protein-coupled receptors in the regulation

  • Structural basis of adhesion GPCR GPR110 activation by stalk peptide and G-proteins coupling

    October 2022 "Adhesion G protein-coupled receptors (aGPCRs) are keys of many physiological events and A comparison of Gq, Gs, Gi, G12 and G13 engagements with GPR110 reveals details of G-protein engagement Taken together, our study fills the missing information of GPCR/G-protein engagement and provides a framework

  • Therapeutic validation of an orphan G protein-coupled receptor: The case of GPR84

    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

  • GPCR Allostery: Unlock Hidden Mechanisms and Make Smarter Drug Decisions

    Masterclass on GPCR Allostery: Unveiling Techniques to Decode Drug Behavior – July 31st, 2025. Welcome back GPCR fans, If your drug discovery strategy still relies on static GPCR models, you’re already behind. Allostery isn’t just an advanced concept—it’s essential to understanding efficacy, ligand bias, and receptor behavior in real-world systems. That’s exactly what Terry’s Corner delivers this week: high-impact insight into GPCR allostery, crafted for pharmacologists and biotech scientists who need to translate mechanistic nuance into better decision-making. 🔍 This Week in Premium: Sneak Peek Industry insights:  Strategic biotech alliances (Chemspace/Enamine, Superluminal Medicines), Novartis financial leadership shakeup, and next-gen GPCR targeting platforms reshaping immunotherapy pipelines. Upcoming events:  GPCR-UK Network Meeting, neuroGPCR symposium, and Transatlantic ECI GPCR event—where discovery and collaboration intersect. Career opportunities:  Exclusive pharma and academic listings you won’t find on job boards—curated for translational scientists and GPCR specialists. Must-read publications:  CXCL12 dimer impact on AML migration, mechanosensitive behavior in GPCRs, and in vivo APLNR biosensor imaging. Terry's Corner : Stop Chasing Affinity and Start Reading the System In this week’s cornerstone Terry’s Corner lecture, Dr. Terry Kenakin reframes GPCRs as dynamic, allosteric sensors—far from static binding sites. This is the lens that lets scientists anticipate drug effects, decode kinetic behavior, and optimize probe-dependent signaling. What you’ll learn: Reveal cryptic binding sites and time-dependent interactions.  Some drugs take hours to reach equilibrium—not because of poor design, but because the system is fluid. Learn how to decode that fluidity. Exploit probe dependence to shape precision pharmacology.  Want to avoid off-target effects? Understand how GPCRs react differently depending on the probe. Map dynamic receptor behavior to real-time decision-making.  Allostery is not passive—it’s predictive. Leverage this model to stay ahead of therapeutic complexity. To stay in the know on upcoming courses and AMA session, get the complementary Kenakin Brief , the weekly newsletter delivered directly to your inbox. Sharpen your discovery decisions ➤ GPCR Signal Transduction Call for Papers: Define What Comes Next Volume I was just the beginning with over 28K reads. As the GPCR field surges forward—from ligand bias to signaling diversity—the guest editors Dr. Lauren Slosky, Stuart Maudsley and Yamina Berchiche invite your insights for Volume II. This is a chance to shape the next scientific consensus on how GPCRs work, signal, and fail. Why this matters: Secure your voice in the next chapter of GPCR science.  Your work belongs in the core conversation—not buried in supplementary files. Position your research for maximum visibility.  This is where funders, peers, and biotech scouts are watching. Contribute to an evolving field still rich with firsts.  Volume II isn’t about repetition—it’s about redefining signal transduction. 📝 Manuscript summary deadline: 23 Sept 2025 📄 Submission deadline: 11 Jan 2026 Submit to Volume II ➤ Discovery On Target: Where the Next Decade of GPCR Drugs Begins If you’re not attending the GPCR-focused sessions at Discovery On Target 2025, you’re missing where the field is headed. It’s the 20th anniversary—and the spotlight is squarely on kinetic modeling, allosteric frameworks, and targeting the “undruggable.” 🔥 Featured:  Dr. Terry Kenakin on “The Kinetics of Allostery: The Added Benefits of Allosteric Function.” Why you need to be there: Learn how kinetic nuance shapes ligand design.  Don’t just measure residence—understand it. Access peer insights on allosteric modulators and biased ligands. Join the conversation on computational targeting and next-gen selectivity. Register for Discovery On Target ➤ What our community is saying “I enjoy the breadth of questioning that goes beyond just the science, and reveals a bit about the scientists as individuals/mentors/people.” — Dr. GPCR Podcast Listener Why Dr. GPCR Premium Membership Gives You an Edge Premium delivers curated, noise-free intelligence every week: deep-dive expert lectures, classified industry news, priority event alerts, job opportunities, and insider commentary—designed to help you move faster, smarter. If you work on GPCRs across translational pharmacology, drug development, or molecular pharmacology, this is your decision advantage. Our Premium Members don’t have to chase signals—they act on them. FAQ: What You Get with Dr. GPCR Premium 🔹 What’s included? The complete Weekly News digest, curated jobs, upcoming events, classified GPCR publications, exclusive on-demand expert frameworks, and member-only discounts. 🔹 Who is it for? GPCR scientists, translational pharmacologists, biotech drug discovery teams, and decision-makers who need fast, curated, career-relevant intelligence to stay ahead. 🔹 Why now? The pace of GPCR innovation is accelerating. Those acting on the right signals today will shape tomorrow’s breakthroughs—and avoid delays others won’t see coming. 👉 Access all the news and upcoming events ➤ 👉 Already a Premium Member?  Read the Full Edition here ➤

  • The sixth transmembrane region of a pheromone G-protein coupled receptor, Map3, is implicated in ...

    The sixth transmembrane region of a pheromone G-protein coupled receptor, Map3, is implicated in discrimination type depends on the molecular recognition of two peptidyl mating pheromones by their corresponding G-protein First, we switched GPCRs between S. pombe and the closely related species Schizosaccharomyces octosporus , which showed that SoMam2 (Mam2 of S. octosporus) is partially functional in S. pombe, whereas SoMap3 (Map3 of S. octosporus) is not interchangeable.

  • GPCR Happy Hour – Boston, Sept 2025

    The company has long-standing expertise in G protein–coupled receptor (GPCR) biology—one of the most

  • G protein-coupled receptors that influence lifespan of human and animal models

    In this sense, G protein-coupled receptors (GPCRs) may be a good option to try to prolong our life while

  • Cell-Type-Specific Effects of the Ovarian Cancer G-Protein Coupled Receptor (OGR1) on Inflammation..

    September 2022 Cell-Type-Specific Effects of the Ovarian Cancer G-Protein Coupled Receptor (OGR1) on Proton-sensing G-protein coupled receptors are activated by acidic environments, but their role in fibrosis Here, we report that the Ovarian Cancer G-Protein Coupled Receptor1 (OGR1 or GPR68) has dual roles in

  • The complicated lives of GPCRs in cardiac fibroblasts

    October 2022 "The role of different G protein-coupled receptors (GPCRs) in the cardiovascular system

  • Opposite Effects of Src Family Kinases on YAP and ERK Activation in Pancreatic Cancer Cells...

    Previously, we identified potent positive crosstalk between insulin/IGF-1 receptors and G protein-coupled The results provide rationale for considering a combination(s) of FDA-approved SFK (dasatinib) and MEK

  • Adrenal G Protein-Coupled Receptors and the Failing Heart: A Long-distance, Yet Intimate Affair

    Synthesis and release of these hormones in the adrenals is tightly regulated by adrenal G protein-coupled

  • Synaptic integration of subquantal neurotransmission by co-localized G protein coupled receptors in

    Ca2+ In combination these pathways allow complex presynaptic integration.SIGNIFICANCE STATEMENTTwo G

  • GPCR Signaling and mTORC1 Regulation

    this review, we will discuss the regulation of mTORC1 by upstream stimuli, with a specific focus on G-protein

  • Functional molecular switches of mammalian G protein-coupled bitter-taste receptors

    Bitter taste receptors (TAS2Rs) are a poorly understood subgroup of G protein-coupled receptors (GPCRs

  • The mouse cytomegalovirus G protein-coupled receptor homolog, M33, coordinates key features of ...

    The mouse cytomegalovirus G protein-coupled receptor homolog, M33, coordinates key features of in vivo signalling repertoire Common to all cytomegalovirus (CMV) genomes analysed to date is the presence of G Constitutive G protein-coupled M33 signalling is required for these phenotypes, although the contribution IMPORTANCE G protein-coupled receptors (GPCRs) act as cell surface molecular "switches" which regulate

  • The Perils and Guardrails of Modifying Signalling Proteins in Bioassays

    Yamaguchi S, Kaneko M, Narukawa M. Liu S, Anderson PJ, Rajagopal S, Lefkowitz RJ, Rockman HA. Lu S, He X, Ni D, Zhang J. Shen S, Zhao C, Wu C, Sun S, Li Z, Yan W, et al. Teng X, Chen S, Wang Q, Chen Z, Wang X, Huang N, et al.

  • G protein-coupled receptor kinase type 2 and β-arrestin2: Key players in immune cell functions...

    August 2022 G protein-coupled receptor kinase type 2 and β-arrestin2: Key players in immune cell functions and inflammation "G protein-coupled receptor kinase type 2 (GRK2) and β-arrestin2 are representative proteins that regulate the transduction and trafficking of G protein-coupled receptor (GPCR) signaling

  • Microbial Metabolites Orchestrate a Distinct Multi-Tiered Regulatory Network in the Intestinal Epith

    September 2022 Microbial Metabolites Orchestrate a Distinct Multi-Tiered Regulatory Network in the Intestinal Epithelium That Directs P-Glycoprotein Expression "P-glycoprotein (P-gp) is a key component of the intestinal epithelium playing a pivotal role in removal of toxins and efflux of endocannabinoids to prevent excessive inflammation and sustain homeostasis. Recent studies revealed butyrate and secondary bile acids, produced by the intestinal microbiome, potentiate the induction of functional P-gp expression. We now aim to determine the molecular mechanism by which this functional microbiome output regulates P-gp. RNA sequencing of intestinal epithelial cells responding to butyrate and secondary bile acids in combination discovered a unique transcriptional program involving multiple pathways that converge on P-gp induction. Using shRNA knockdown and CRISPR/Cas9 knockout cell lines, as well as mouse models, we confirmed the RNA sequencing findings and discovered a role for intestinal HNF4α in P-gp regulation. These findings shed light on a sophisticated signaling network directed by intestinal microbial metabolites that orchestrate P-gp expression and highlight unappreciated connections between multiple pathways linked to colonic health." Read more at the source #DrGPCR #GPCR #IndustryNews

  • Inversago Pharma appoints Glenn S. Vraniak as Chief Financial Officer

    biotech company with a unique portfolio of CB1 inverse agonists, today announces the appointment of Glenn S. Vraniak served as Chief Financial Officer of Evaxion Biotech A/S, an AI enabled immuno-oncology company

  • Obesity-induced changes in human islet G protein-coupled receptor expression: Implications for ...

    Obesity-induced changes in human islet G protein-coupled receptor expression: Implications for metabolic regulation G protein-coupled receptors (GPCRs) are a large family of cell surface receptors that are

  • G protein-coupled receptor kinase 2 is essential to enable vasoconstrictor-mediated arterial ...

    G protein-coupled receptor kinase 2 is essential to enable vasoconstrictor-mediated arterial smooth muscle production and circulation of vasoconstrictors, resulting in enhanced signalling through their cognate G In VSMC, G protein-coupled receptor kinase 2 (GRK2) is known to regulate numerous vasoconstrictor GPCRs

  • The Imprecision Problem: Why Your GPCR Drug Discovery Program Is Off-Track Before It Even Starts

    Unlocking the Puzzle: The Importance of Precision in GPCR Programs and the Hidden Costs of Overlooking Details. A GPCR program can have world-class science, top-tier talent, and millions in funding — and still fail. Not because the science is wrong. Not because the people aren’t brilliant. But because the program is run on duct tape and heroics instead of precision. Your program isn’t slipping because of bad science — it’s bleeding money because your systems were broken before the first experiment ran. And every time your Head of Biology spends each night copy-pasting data instead of thinking about the next experiment, your program is bleeding six figures in lost time and wasted salaries. Brilliant minds doing low impact work is not a strategy. It’s a slow-motion car crash. Hiring Won’t Save Your GPCR Drug Discovery Program When a drug discovery program stalls, the default reflex is always the same: hire more people. Bring in a computational chemist. Add a data scientist. Surely more hands will move the needle. But here’s the reality: even ultra-specialized experts can’t fix systemic dysfunction in their spare time. They’re hired for science, not for building operational scaffolding. And when you chain your highest-paid scientists to repetitive admin work, you’re not solving problems — you’re multiplying them. Every two-week delay in a DMTA cycle can burn through hundreds of thousands in salaries and overhead. That’s not a hiccup. That’s a hemorrhage. Bad Data Management Is Undermining Your GPCR Drug Discovery Team The real problem isn’t competence. It’s the absence of operational precision. Even flawless experiments collapse under sloppy systems. A few familiar failure points: Fragmented Data: GPCR programs spew data across files, folders, and inboxes. Without a unified drug discovery data management  pipeline, teams waste hours cleaning, reconciling, and integrating before they can even think about analysis. A good ELN that pipes instrument outputs into a central hub — where QC, analysis, consumption and consolidation across assays — isn’t a luxury. It’s oxygen. Undefined Protocols: “We’ll figure it out” is not a workflow. Without clear rules of engagement, communication becomes chaos, progress gets lost in Slack threads, and insights die in inboxes. Ambiguous Decision Gates: Molecules advance or stall based on vibes, not criteria. That leads to premature investment in weak scaffolds or endless tinkering with dead ends. These aren’t minor oversights. They’re cracks in the foundation. And cracks don’t stay small for long. Build Precision Systems for GPCR Drug Discovery The only way out for GPCR drug discovery programs isn’t more people or shinier assays. It’s a deliberate blueprint for precision. This doesn’t mean an overnight overhaul. It means a commitment to continuous improvement — starting with the highest-friction gaps and working upward. Plan, fix at the root, and stop fighting the same fire every week. The payoff? Progress that’s predictable, not reactive. The Hidden Costs of Poor Drug Discovery Data Management Stop pretending more hires or new assays will save you. They won’t. Every DMTA cycle lost to fragmented data and sloppy processes costs your company hundreds of thousands of dollars. That’s not “part of the process.” That’s a chaos tax — and you’re paying it in cash, time, and morale. If you want your program to survive, you need a Blueprint for Precision. Not next quarter. Not after the next fire drill. Now. Because the truth is harsh: in drug discovery, you don’t run out of science. You run out of money. And if your systems aren’t built for precision, you’ll run out fast. 👉 In Part 2, we’ll expose exactly how fragmented data cripples GPCR programs — and how to fix it before it sinks yours. And if you’re already seeing the cracks? Don’t wait for Part 2. Reach out. Let’s build the systems now, before the next delay burns another half a million. 🚀 Book your free 30-minute precision audit — before your next DMTA cycle costs another $200K Let’s unlock the momentum your GPCR program needs. 👉 https://calendly.com/drgpcr/yamina-corner Or explore how we can work together: 👉   Yamina.org

  • Role of G Protein-Coupled Receptors in Hepatic Stellate Cells and Approaches to Anti-Fibrotic ...

    Role of G Protein-Coupled Receptors in Hepatic Stellate Cells and Approaches to Anti-Fibrotic Treatment G protein-coupled receptors (GPCRs) are cell surface receptors that mediate the function of a great variety

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