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  • Perkins’ Head of Molecular Endocrinology and Pharmacology, Professor Kevin Pfleger, was appointed...

    December 2021 Perkins’ Head of Molecular Endocrinology and Pharmacology, Professor Kevin Pfleger, was

  • 📰 GPCR Weekly News, September 11 to 17, 2023

    Kevin Wright on his new position as Director of Targeted and Immuno-oncology at GPCR Therapeutics, our Kevin Wright Joins GPCR Therapeutics as Director of Targeted and Immuno-oncology Sosei Heptares Adds

  • Dr. Kevin Pfleger and Dr. Elizabeth Johnstone were awarded one of the 2022 Diabetes Research...

    Kevin Pfleger and Dr. "Congratulations to Perkins Professor Kevin Pfleger and Dr Elizabeth Johnstone who were awarded one of

  • Mechanism vs. Assumption: A Model-First Path to Getting GPCR MoA Right

    & GPR3 regulated by a negative allosteric modulator Terry's Corner – Determine GPCR MoA Early (and Right Those acting on the right signals today will shape tomorrow’s breakthroughs—and avoid delays others won

  • 🤯Mind-blowing GPCR Scoops! Discover the Latest Breakthroughs! ⦿ Nov 18 - 24, 2024

    adenocarcinoma, β-blockers and antihistamines: A clinical trial is needed Jillian G Baker ,  Erica K Sloan ,   Kevin

  • How Advanced GPCR Kinetics Sharpen Decision Making (and Save You Time)

    Industry insights:  Orforglipron’s trajectory is redefining weight-management and diabetes markets—implications This week, you will learn how to confirm equilibrium the right way, detect time-dependent occupancy and Learn how to choose fluorophores (brightness, stability, spectra), reduce background (far-red/near-IR Scale confidently:  Use bright, stable ligands for HTS and bias profiling. Those acting on the right signals today will shape tomorrow’s breakthroughs—and avoid delays others won

  • Innovative Data-Driven Solutions: The pHSense Revolution

    These probes shift brightness and fluorescence lifetime as pH changes. They learned how to fine-tune both brightness and fluorescence lifetime. You’re just changing how bright it is—and how long it glows,” said Dr. Eric Trinquet. They constructed the platform, tested every variable—pKa, brightness, lifetime—and made decisions that “You start wide with chemistry, you narrow with biology, and at the end—if you did it right—you open

  • The Perils and Guardrails of Modifying Signalling Proteins in Bioassays

    For the serotonin 5-HT2A receptor (5-HT2AR) with the Gαi/o family of transducers, Wright and colleagues narrowed the activation of Gαi/o protein subtypes from all except Gαi1 to only Gαz in a recent study by Wright Wright and colleagues [36] showed that these heterotrimer-based biosensors for the 5-HT7A/B receptors 5-HT2A receptor (5-HT2AR), and (C) muscarinic acetylcholine M3 receptor (M3R) in a recent study by Wright Wright SC, Avet C, Gaitonde SA, Muneta-Arrate I, Le Gouill C, Hogue M, et al.

  • Orthosteric vs Allosteric Interactions— and the pHSense Shift in Internalization

    By carefully tuning both brightness and fluorescence lifetime, they engineered a two-dimensional pH response “You’re changing how bright it is—and how long it glows.” – Advantages of Fluorescent Ligands in CNS GPCR Drug Discovery In neuroscience drug discovery, the right tool  can be just as critical as the right target . Acting on the right signals today shapes tomorrow’s breakthroughs—and avoids slowdowns others won’t see

  • Fluorescence based HTS compatible ligand binding assays for dopamine D3 receptors in baculovirus preparations and live cells

    The Log(IC50) change in time was fitted with equation  3  and k given is the weighted average from 3  (A)  or 4  (B)  experiments with weighted SD The Ki values were calculated based on the IC50 values, Fluorescence and bright-field images of total (left panels) and non-specific binding (central panels) of CELT-419 to live HEK293-D3R cells and to SKOV3 cells without D3 receptors (right panels). The contrast of fluorescence and bright-field images was enhanced for presentation purposes only, the

  • Assay Sensitivity: The Hidden Lever Driving GPCR Drug Discovery

    Assay sensitivity is like adjusting the brightness on a microscope—set it right, and hidden details jump What emerges is not just more data—it’s the right data, positioned to inform strategic decision-making

  • Molecular creativity in drug discovery

    Breakthroughs this week:  Orphan receptor GPRC5B in neurogenesis; Septerna’s pill-based weight-loss strategy Those acting on the right signals today will shape tomorrow’s breakthroughs—and avoid delays others won

  • From Snapshots to Predictions: Why Mechanism of Action Matters

    Without the right model, it’s like staring at identical twins—you can’t tell them apart until you see With the right model, you can separate lookalikes and prevent an entire program from being misclassified Here’s the uncomfortable truth: you can never prove a model “right.” They need the right data . Only when the data were fit to the right model did the picture snap into focus.

  • Reflections on My PhD Journey: Lessons Learned

    Choosing the Right Lab The lab you choose plays a pivotal role in shaping your PhD journey. However, with multiple great options, choosing the right lab wasn't easy. The right environment, paired with a supportive supervisor, laid the foundation for a fulfilling and The Role of Mentors and Supervisors Having the right mentor is indispensable for a successful PhD journey

  • Competitive vs Non-Competitive GPCR Antagonists: How to Interpret Pharmacology Data with Confidence

    lipid droplets; novel atypical GPCR-arrestin complexes; Lilly's oral GLP-1, orforglipron, delivers weight Gain a competitive edge by asking the right questions about binding kinetics and experimental constraints Those acting on the right signals today will shape tomorrow’s breakthroughs—and avoid delays others won

  • How Understanding Intracellular Drug Access Can Transform Your GPCR Drug Discovery Program

    teams and scientists, staying ahead requires more than just reading papers—it demands access to the right the key insights and opportunities that are shaping the future of GPCR research and drug discovery right The right information at the right time can mean the difference between a breakthrough and a dead end Those acting on the right signals today will shape tomorrow’s breakthroughs—and avoid delays others won

  • From GPCR Data Chaos to Decisive Action

    Not possible when nothing’s built to surface the right  insights early. I know how to ask the right scientific questions—and when to shift from analysis to execution. decisive action ✅ This is hands-on support —not passive advising p.s: Still unsure if this is the right

  • Curve Shifts Don’t Lie, But Your Eyes Might

    By the end, you’ll know how to choose the right test, design experiments with power built in, and validate ability to calculate how many replicates you really  need for 95% confidence ✅ Tools to choose the right Specifically, you’ll be able to: Design experiments with the right replicate count to balance rigor and With the right methods, you’ll know (not hope) that your results are real, reproducible, and actionable

  • Unlock the Hidden Lives of Receptors – Are You Ready?

    With the right lens, you’ll see why efficacy is more than signal strength: it's a fingerprint of conformational

  • Misread the Curve, Misjudge the Drug: Rethinking Antagonism in GPCR Pharmacology

    Why Misreading Antagonism Delays GPCR Drug Discovery If a dose-response curve shifts to the right, you DR curves shift to the right with no loss of maximal effect. One shifts neatly to the right without dropping the maximum.

  • Adhesion GPCR Consortium Newsletter - May 2024

    Thomas Südhof, but did not start working on them right away. AB: The next workshop will likely bring together some of the hottest adhesion GPCR research going on right The meat on a rotating spit with its bright red/orange chili-based marinade (spicy but not hot) catches

  • Specific Functions of Melanocortin 3 Receptor (MC3R)

    In addition to its function about weight gain and appetite control mechanisms of MC3R, recent studies aimed to point out the importance of the MC3R regulations in three main concepts: 1) its impact on weight

  • Discover the Hottest GPCR News of the Week: Oct 7-13, 2024!

    Ready for your GPCR quest, so bold and bright? Join us now, and let's explore with all our might! in Neuroscience Ventral tegmental area amylin / calcitonin receptor signaling suppresses feeding and weight

  • 📰 GPCR Weekly News, June 17 to 23, 2024

    Shane Wright, Michel Bouvier, et al., for their work on Conformation- and activation-based BRET sensors

  • Your GPCR Program Decisions Depend on Good Data Interpretation

    GPCR , we’re focusing on the hidden risks that undermine progress and how the right frameworks can keep GPCR Premium is designed for scientists who need the right intelligence, fast—without noise, distractions Those acting on the right insights now will define the next wave of discovery.

  • Accelerating GPCR Drug Discovery: What 40 Years of Pharmacology Reveal

    GPCR programs stall  not because the target was wrong, but because teams waited too long to test the right Early In Vivo Wins the Race When is the right time to move beyond cell assays? you get your molecule in vivo, the sooner you know whether anything’s happening—and whether it’s the right

  • Dr. GPCR Updates

    With the right tools, bold ideas, and powerful collaborations, you’re not just keeping pace.

  • Science Needs Rigor, But Also Joy

    communicates under pressure • Space for curiosity, humor, and human connection For anyone searching for the "right

  • A Setmelanotide-like Effect at MC4R Is Achieved by MC4R Dimer Separation

    Due to increasing numbers of people with excess body weight, the MC4R has become a target of interest setmelanotide, a novel synthetic MC4R agonist, suggest a predominant role of the Gq/11 pathway regarding weight

  • Identification and functional characterization of the sulfakinin and sulfakinin receptor in the...

    knock down SK and SKR reduced the transcription levels of the target genes and increased their body weight In parallel, injection of SK caused a significant reduction in body weight and increase in mortality

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