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

    Elizabeth Johnstone were awarded one of the 2022 Diabetes Research Grants at the World Diabetes Day Breakfast Perkins Professor Kevin Pfleger and Dr Elizabeth Johnstone who were awarded one of the 2022 Diabetes Research This $60,000 grant from Diabetes Research WA will assist the Perkins' Molecular Endocrinology and Pharmacology

  • Is Your GPCR Drug Discovery Program Built for Breakthroughs or Breakdowns?

    Tackling the GPCR Imprecision Problem: Strategic Planning for Sustainable Progress in Complex Systems. In the high-stakes world of GPCR drug discovery , breakthrough science isn't enough. You can have the most brilliant minds and cutting-edge assays, but if your science isn't continuously integrated with your GPCR operational strategy and investment goals, even the most promising program can falter. This fundamental disconnect between the lab and the boardroom  is precisely where programs get stuck—not because of bad science, but because companies find themselves throwing more money and people at problems that could be solved with better systems. This reactive approach, driven by a "go fast" mindset, burns through precious capital and time, leaving both scientific teams and investors frustrated. Companies find themselves throwing more money and people at problems that could be solved with better systems . This reactive approach, driven by the prevailing wisdom of "going fast" and focusing only on the science, burns through precious capital and time, leaving both scientific teams and investors frustrated. This belief that we don't have time to build better systems is a costly miscalculation. It reminds me of a conversation I recently overheard: my oldest child complaining about having to do 'everything at the same time ,' only for the youngest to wisely respond, 'No, you just need to do one thing at a time .' This simple truth applies profoundly to the "go fast" culture in biotech. We believe we don't have time to build better systems, but in reality, our most brilliant and expensive minds are stuck with low-impact tasks due to a lack of systems thinking . My perspective on this challenge is shaped not by a 40-year journey at the bench, but by an expertise in systems thinking  and operational discipline . My work isn't just  about the latest and best assay; it's about the framework that ensures the right assay data leads to the right decision. This is the critical piece that often gets lost in the "go fast" culture—the integration of science with strategy and flawless execution. I’ve lived this firsthand, not just in theory, but by building these systems from the ground up. I understand that embracing a systematic approach can feel daunting, especially with the pressure to move quickly. At Dr. GPCR, we recognized this core problem. Our Chief Brainstorm Officer, Attila Foris , is building a system so transparent that anyone joining the company can integrate seamlessly. Every time a problem arises, we trace it back to its root cause, implementing changes that prevent its recurrence. This iterative process of continuous, planned improvement ensures you're always addressing the next critical area. This is the essence of de-risking GPCR programs through operational excellence. This kind of continuous improvement doesn't happen organically; it demands intentional planning and a systematic approach, ensuring every step forward is strategic and sustainable. The Role of Systems Thinking in GPCR Drug Discovery Systems thinking is the intentional practice of seeing the entire GPCR program as a single, interconnected entity. It's the opposite of a reactive approach, where problems are solved in isolation. It’s the fundamental framework for building your Precision Blueprint , ensuring every scientific detail, operational process, and strategic decision aligns to create a seamless, predictable pathway to success. What You'll Learn in This Series Over the next five bi-weekly installments, " The GPCR Precision Blueprint " series will unpack how to bridge this critical gap. I'll show you how to transform your drug discovery process from a series of disconnected efforts into a seamless, predictable, and de-risked pathway. Part 1: The GPCR Imprecision Problem : I'll reveal why reliance on hiring more people over investing in robust systems thinking  is a multi-million dollar mistake. We'll look at how overlooked operational details, such as misaligned data from diverse GPCR assay types or communication gaps in cross-functional collaboration , lead to critical costs. Part 2: The Data Disconnect : Discover how fragmented, unmanaged GPCR data  cripples scientific progress and strategic decision-making. Learn how to build an integrated data pipeline  that transforms this chaos into a strategic asset. Part 3: The Financial Friction : Explore how a lack of precise alignment between GPCR scientific milestones  and financial realities creates significant risk. Learn to tie your program's progress directly to your funding runway, incorporating crucial early commercial and medical foresight. Part 4: The Investor Imperative : Understand what investors truly prioritize beyond just great science. Learn to translate your program’s internal operational precision into a compelling, de-risked narrative  that builds confidence and secures critical venture capital . Part 5: Your Precision Blueprint : I'll tie it all together, providing a concise, actionable guide for implementing this holistic approach within your own GPCR operational strategy , emphasizing that precision is a continuous, intentional journey towards predictable success. The GPCR Precision Blueprint is more than a concept. If you're ready to move beyond the articles and build these systems for your own GPCR program, let's connect. I work with biotechs, VCs, and CROs to implement the framework that ensures every step forward is strategic and sustainable, offering precision scientific and operational guidance  to accelerate discovery . 🚀 Book your free 30-minute strategy call Let’s unlock the momentum your GPCR program needs. 👉 https://calendly.com/drgpcr/yamina-corner Or explore how we can work together: 👉 Yamina.org

  • High-Content Screening for GPCR Programs: Overcoming Assay Limitations with Fluorescent Ligands

    High-content screening (HCS) has become a cornerstone in GPCR and phenotypic drug discovery, enabling researchers The resulting multiparametric datasets are well-suited for GPCR research, where receptor trafficking, Non-Radioactive Workflow By removing isotopes, researchers gain safer, more scalable, and more environmentally For teams working in GPCR pharmacology or cannabinoid research, these tools accelerate hit validation At Celtarys, we remain committed to enabling this transition and supporting researchers as they design

  • In vivo detection of GPCR-dependent signaling using fiber photometry and FRET-based biosensors

    Hence, it has wide applicability across a spectrum of neuroscience research, ranging from the study of

  • TRPM3 in the eye and in the nervous system - from new findings to novel mechanisms

    August 2022 "The calcium-permeable cation channel TRPM3 can be activated by heat and the endogenous steroid pregnenolone sulfate. TRPM3's best understood function is its role as a peripheral noxious heat sensor in mice. However, the channel is expressed in various tissues and cell types including neurons as well as glial and epithelial cells. TRPM3 expression patterns differ between species and change during development. Furthermore, a plethora of TRPM3 variants that result from alternative splicing have been identified and the majority of these isoforms are yet to be characterized. Moreover, the mechanisms underlying regulation of TRPM3 are largely unexplored. In addition, a micro-RNA gene (miR-204) is located within the TRPM3 gene. This complexity makes it difficult to obtain a clear picture of TRPM3 characteristics. However, a clear picture is needed to unravel TRPM3's full potential as experimental tool, diagnostic marker and therapeutic target. Therefore, the newest data related to TRPM3 have to be discussed and to be put in context as soon as possible to be up-to-date and to accelerate the translation from bench to bedside. The aim of this review is to highlight recent results and developments with particular focus on findings from studies involving ocular tissues and cells or peripheral neurons of rodents and humans." Read more at the source #DrGPCR #GPCR #IndustryNews

  • Single-molecule counting applied to the study of GPCR oligomerization

    October 2022 "Single-molecule counting techniques enable a precise determination of the intracellular abundance and stoichiometry of proteins and macromolecular complexes. These details are often challenging to quantitatively assess yet are essential for our understanding of cellular function. Consider G-protein-coupled receptors-an expansive class of transmembrane signaling proteins that participate in many vital physiological functions making them a popular target for drug development. While early evidence for the role of oligomerization in receptor signaling came from ensemble biochemical and biophysical assays, innovations in single-molecule measurements are now driving a paradigm shift in our understanding of its relevance. Here, we review recent developments in single-molecule counting with a focus on photobleaching step counting and the emerging technique of quantitative single-molecule localization microscopy-with a particular emphasis on the potential for these techniques to advance our understanding of the role of oligomerization in G-protein-coupled receptor signaling." Read more at the source #DrGPCR #GPCR #IndustryNews

  • Luciferase-based GloSensor™ cAMP assay: Temperature optimization and application to cell-based kinet

    August 2022 Luciferase-based GloSensor™ cAMP assay: Temperature optimization and application to cell-based kinetic studies "G protein-coupled receptors (GPCRs) are an important receptor superfamily and common therapeutic targets. The second messenger cyclic adenosine monophosphate (cAMP) is a key mediator in many GPCR signaling pathways. Monitoring intracellular cAMP levels can help identify orthosteric agonists and antagonists, as well as allosteric modulators. In this regard, luminescence-based biosensors have revolutionized our ability to monitor GPCR signaling kinetics. The GloSensor™ cAMP assay enables real-time monitoring of signaling downstream of many GPCRs. However, it is crucial to optimize assay conditions such as temperature. As well, it has not been reported whether the effects of temperature on biosensor activity are reversible. Here, we describe the temperature sensitivity and reversibility of the GloSensor™ cAMP assay, and which GloSensor™ version is optimal for measuring cytosolic cAMP. We also present a detailed protocol for monitoring cAMP levels in live cells expressing endogenous or exogenous GPCRs. Temperature optimization studies were carried out using HEK293H cells transiently transfected with the adenosine receptor A2a and the GloSensor™ plasmid (pGloSensor-20F or -22F). We found that preincubation and luminescence reading at room temperature were optimal as compared to higher temperatures. As well, the GloSensor-22F biosensor had a superior signal-to-background ratio and the effect of temperature on biosensor activity was reversible. However, thermal instability of the biosensor may pose a problem for in vivo studies. Nevertheless, the GloSensor™ cAMP assay can be applied to analyze signaling by a wide range of GPCRs for drug discovery" Read more at the source #DrGPCR #GPCR #IndustryNews

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

    Exploring Intracellular Targets: Bridging the Gap Between In Vitro and In Vivo GPCR Research - August and a research associate/scientist in in vitro pharmacology. GPCR Podcast : The Future of GPCR Drug Discovery with Molecular Modeling The field of GPCR research is research within the field of Cellular Biochemistry. Discover the research topic ➤ Why Dr.

  • Inside Out: Mapping GPCRs from Membrane Codes to Market Moves

    studies reveal how phosphorylation barcodes shape arrestin engagement, a biased NTSR1 modulator targets pain Barcodes Shape Arrestin Engagement with ACKR3   A β-Arrestin-2-Biased NTSR1 Modulator for Non-Addictive Pain Explore this week’s research, tools, and biotech insights in one place.

  • APEX2/AUR Biosensor: A Powerful Tool for Protein Interaction and Trafficking

    The research team, led by Brandon Novy and colleagues, utilized an innovative APEX2/AUR biosensor that By employing this biosensor, the research team identified 492 genes that significantly influence DOR After the labeling reaction, the researchers purified and biotinylated proteins (those that have been As the opioid crisis continues to challenge public health, insights gained from this research could inform The implications of this research extend beyond basic science ; understanding the role of DNAJC13 in

  • 🎄 Have Yourself a Merry Little GPCRmas! ❄ Dec 9 - 15, 2024

    As researchers, we all understand the importance of data in driving meaningful discoveries  and advancing guide us in tailoring resources , tools , and content to meet your needs better and help fuel your research Pharmacological Society Vane Medal and switching on the Christmas lights at the University of Glasgow Advanced Research Scientist, Medicinal Chemistry PhD fellowship in GPCR mechanosensing Senior Scientist, GPCR Pharmacology Research differential endoplasmic reticulum environment amongst neuronal subtypes Methods & Updates in GPCR Research

  • Exploring pharmacological inhibition of G q/11 as an analgesic strategy

    Previous research showed that activation of Gq/11 proteins by G-protein coupled receptors has pro-nociceptive properties, suggesting that blockade of Gq/11 signalling could be beneficial for pain control. Experimental approach: We used a series of behavioural assays to evaluate the acute responses of mice to painful

  • GPR125 (ADGRA3) is an autocleavable adhesion GPCR that traffics with Dlg1 to the basolateral...

    that contains various adhesion-related domains and a highly-conserved GPCR-autoproteolysis-inducing (GAIN The cleavage appears to occur at an atypical GPCR proteolysis site within the GAIN domain during an early

  • Targeting GPCRs in the CNS: Advances in Drug Discovery Strategies

    The activation of these pathways regulates pain modulation, memory consolidation, motor coordination neuroprotective functions and is now being investigated for its role in Parkinson’s disease and neuropathic pain Of the traditional GPCRs, CBRs are gaining ground as potential therapeutic targets in several CNS diseases More research into the endocannabinoid system (ECS) will let us access these GPCRs in a safer manner

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

    Fluorescent probes illuminate the mysteries of GPCRs in cutting-edge research. God Molecule"; Novo Nordisk looks to next generation of obesity, diabetes drugs with $550M Replicate research Career opportunities:  Research Assistant; Postdoctoral Associate; Senior Scientist, Data Science—curated Must-read publications:  β-arrestin2-biased allosteric modulator for pain beyond opioids & GPR3 regulated Join Terry's Corner Today ➤ Celtarys Research – Confocal Imaging That Preserves GPCR Function Confocal

  • Targeted Therapies to Reduce Side Effects in Modern Drug Development

    The sheer complexity of the cell and the astonishing diversity of diseases are just two reasons why researchers drawback of causing damage to healthy cells in the process, leading to side effects that can include pain Nevertheless, researchers have a host of new technologies at their disposal to develop targeted therapies

  • 📰 GPCR Weekly News, June 3 to June 9, 2024

    take a moment to explore our most recent coverage of GPCRs this week, which includes 15 insightful research Stay informed with the most recent developments in GPCR research and industry news. Join the global GPCR community to present your research—submit your abstract using this form. function in autophagy control: a systematic approach of chemical intervention Methods & Updates in GPCR Research Scientist, In vitro pharmacology Senior Scientist - Receptor Pharmacology Postdoctoral Scientist Senior Research

  • 📰 GPCR Weekly News, March 27 to April 4, 2023

    Methods & Updates in GPCR Research Discovery and design of G protein-coupled receptor targeting antibodies Fourth Quarter and Full Year 2022 Financial Results and Recent Highlights Salipro Biotech publishes research July 2 - 7, 2023). 3rd Annual Meeting IRN I-GPCRNet (October 25 - 27, 2023) GPCR Jobs NEW Convergent Research - Senior Scientist, Cell-Based Assay Development NEW Post Doctoral Fellow NEW Research associate in protein production NEW Vice President, Oncology Clinical Research NEW PostDoctoral Associate NEW PostDoctoral

  • 📰 GPCR Weekly News, April 15 to 21, 2024

    This week, we have a comprehensive coverage of 12 GPCR research papers. This week's highlight includes congrats to: Luca Franchini and Cesare Orlandi for their research on Deorphanization Submit a few slides for a poster presentation to showcase your research and network with our community metamorphosis and spawning behavior in Pacific abalone The role of orphan G protein-coupled receptors in pain Research Technologist I Senior Scientist- Internal Medicine Research Unit Postdoctoral Scholar – Synaptic

  • Unlock the Future of GPCR Science: Breakthroughs and Courses Await | Sep 2 - Sep 8, 2024

    Hello GPCR Enthusiasts, Dive into this week's exciting updates on cutting-edge GPCR research, new learning Protein-Coupled Receptors for New Therapeutic Options 📍  Boston, MA 📅 October 2 -3, 2024 Join top researchers Europe July 12 - 17, 2026 | 20th World Congress of Basic and Clinical Pharmacology GPCR Jobs HIGHLIGHT Research Scientist, Computational Chemistry Postdoc in GPCR mechanosensing   Postdoctoral Position Postdoctoral research Therapeutic Targets for the Treatment of Neurological Disease s Activation of GPR55 alleviates neuropathic pain

  • The Hidden Driver of GPCR Drug Success: Why Target Residence Time Matters More Than You Think

    , This week's breakthroughs are crucial for staying ahead in the rapidly evolving landscape of GPCR research Career opportunities:  Explore a selection of high-level job openings in high-throughput screening, research Catherine’s research, blending GPCR signaling studies with public health data, offers critical insights Competitive Edge:  Stay informed on emerging public health threats and the scientific research aimed Shape the next generation of cellular biochemistry research.

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

    This Thursday, explore the latest content on GPCRs, which includes 29 informative research papers and Stay informed about the most recent developments in GPCR research and industry updates. Rajagopal, Robert Lefkowitz, Howard Rockman for their review G Protein-Coupled Receptors: A Century of Research protein-coupled receptor-like proteins in rice (Oryza sativa) G Protein-Coupled Receptors: A Century of Research Assistant Senior Scientist - Receptor Pharmacology Postdoctoral Scientist Senior Research Associate/

  • From Lab Bench to Boardroom: The Unexpected Path of a Medicinal Chemist

    co-founders soon realized, commercializing it was the only way to deliver that value to the broader GPCR research Celtarys Research, now partnering with Dr. GPCR, is helping researchers worldwide gain access to customized, reliable assay tools without the delays science-driven solutions on their company page . _______________ Keyword Cloud:   GPCR drug discovery , GPCR research

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

    Career opportunities:  Roles spanning research associates to principal scientists across membrane proteins From Bench Frustrations to Breakthrough Design For decades, GPCR trafficking research relied on overexpression chemistry can shift the entire GPCR toolkit. 👉 Go behind the scenes with Revvity’s R&D team ➤ Celtarys Research Because they give researchers something rare in CNS work: clarity in complexity. start here 🚀 Join Premium Today & Enjoy ➤ 🎓 Full GPCR University + 🔬 200+ expert talks 🗞️ Weekly research

  • GPCR Buzz of the Week | Sep 23 - 29, 2024

    exceptional professors' ability to simplify the complexity of GPCR pharmacology and apply it to their research Europe July 12 - 17, 2026 | 20th World Congress of Basic and Clinical Pharmacology GPCR Jobs HIGHLIGHT Research Scientist, Computational Chemistry Postdoc in GPCR mechanosensing   Postdoctoral Position Postdoctoral research protein coupled receptor transcripts in human immune cells and platelets Methods & Updates in GPCR Research framework combining molecular image and protein structural representations identifies candidate drugs for pain

  • 📰 GPCR Weekly News, March 25 to March 31, 2024

    This week's highlight includes congrats to: Junyi Liang, Niña Caculitan, and Adam W Smith for their research If you want to showcase your research, you can submit a poster presentation to our community, take advantage 2026 | 20th World Congress of Basic and Clinical Pharmacology 2026 GPCR Jobs Postdoctoral Associate Research Technologist I Senior Scientist- Internal Medicine Research Unit Postdoctoral Scholar – Synaptic physiology , optical imaging, substance use disorder, pharmacology Research Fellow Postdoctoral Fellow – Molecular

  • 📰 Breaking Down the Latest GPCR Discoveries: a Weekly Update (Nov 27-Dec 3, 2023)

    Matthew T Eddy and his team's research on A2A adenosine receptor activation by G protein and mutations protein and fat synthesis GPCRs in Neuroscience Targeting sensory neuron GPCRs for peripheral neuropathic pain proliferation of T-cell lymphoma cells through the enhancement of apoptosis Methods & Updates in GPCR Research Heptares to take back GPCR agonist after GSK changes course All-rounder among receptors inspires drug research scientist – oncology biomarker expert NEW Postdoctoral Fellow NEW Scientific Assistant Scientist Lead Researcher

  • Why Sokhom Pin Never Left GPCRs, Even When Everyone Else Did

    But Sokhom Pin stayed loyal to GPCRs , even when big pharma turned its gaze to other targets like kinases A Career Built on Consistency From CGRP receptor antagonists at BMS to opioid receptor research at Alkermes and early-stage work at Cerevel and Superluminal, Sokhom’s consistency has paid off in ways short-term drug discovery , G protein-coupled receptors , GPCR webinar series , GPCR scientist network , GPCR research

  • Decoding Olfactory GPCRs: How AlphaFold and AI Are Changing the Game

    For most researchers, that’s a dead end. For Alessandro Nicoli, it’s an opportunity. The main challenge was simple but daunting: “The challenge was to get a face to those proteins—the structure —Alessandro Nicoli For the first time, researchers had a reliable set of predicted structures to work —Alessandro Nicoli A New Era of GPCR Research AlphaFold didn’t just fill a gap—it shifted the focus of

  • 📰 GPCR Weekly News, October 30 to November 4, 2023

    inhibits purinergic P2Y2 receptor and TRPV4 to suppress astrocyte activation and to relieve neuropathic pain combination with decitabine in relapsed or refractory acute myeloid leukemia Methods & Updates in GPCR Research Treatment of Insomnia OMass Therapeutics Releases First Protein Structures in PDB, Advances Lupus Therapy Research Structure Therapeutics Receives R&D Achievement of the Year Award for GPCR Research Bryan Roth, Natural | SLAS Europe 2024 Conference and Exhibition June 2 - 7, 2024 | Chemotactic Cytokines GPCR Jobs NEW Research

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