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dynamics ( e.g FLAsH biosensor [11]), cAMP production (e.g CAMYEL assay [12]) , and ERK activity (e.g YEN The ONE-GO biosensors, designed in a single vector, incorporate a G protein tagged with a YFP acceptor Zhou, Y., et al., Multiple GPCR Functional Assays Based on Resonance Energy Transfer Sensors.  Namkung, Y., et al., Monitoring G protein-coupled receptor and β-arrestin trafficking in live cells using

We can’t wait to share it with you! a database of binding sites of human G-protein coupled receptors under diverse states Fan Liu , Han Zhou , Xiaonong Li , Liangliang Zhou , Chungong Yu , Haicang Zhang , Dongbo Bu 🤩 Seriously, why would you As a premium member , you have access to all the complimentary perks as well as: Dr. Get your 5-day free trial TODAY!

proteins (Gether 2000), with numerous intermediate sub-states in between (Vauquelin and Van Liefde 2005; Yao disruption of natural spatial and temporal signaling patterns regulated by physiological systems (Wold and Zhou intervention for metabolic diseases such as liver disease, obesity and diabetes (Secor et al. 2021; Wold and Zhou

Week’s Highlights: SNX9 family mediates βarrestin-independent GPCR endocytosis Valeria Robleto , Ya Zhuo , Joseph Crecelius , Sara Benzow , Adriano Marchese Cannabinoid regulation of angiotensin II-induced GPCR Events You can start planning and save some dates in 2025 . Why, you ask? Get your 5-day free trial TODAY!

Sun D, Gao W, Hu H, Zhou S. Why 90% of clinical drug development fails and how to improve it? Alzheimers Dement (N Y). 2017;3(4):651-657. 11.         Dowden H, Munro J. Yamaguchi S, Kaneko M, Narukawa M. Manchanda Y, ElEid L, Oqua AI, Ramchunder Z, Choi J, Shchepinova MM, et al. González-Maeso J, Weisstaub NV, Zhou M, Chan P, Ivic L, Ang R, et al.

October 2022 Pharmacological targeting of cGAS/STING-YAP axis suppresses pathological angiogenesis and Meanwhile, cGAS deletion upregulated profibrotic Yes-associated protein (YAP) signaling in endothelial , which was evidenced by the attenuation of organ fibrosis in mice specifically lacking endothelial YAP Pharmacological targeting of cGAS/STING-YAP signaling by both a small-molecule STING agonist, SR-717, Further, pharmacological targeting of cGAS/STING-YAP axis exhibits the potential to alleviate liver and

G.; Ishiguro, H.; Horiuchi, Y.; Onaivi, E. S. W.; Wu, Y.; Zhao, S.; Shui, W.; Li, S.; Korde, A.; Laprairie, R. B.; Stahl, E. L.; Ho, J. .; Zhou, H.; Kufareva, I.; Wu, B.; Zhao, Q.; Hanson, M. A.; Bohn, L. V.; Mostinski, Y.; Mach, L.; Wasinska-Kalwa, M.; Weise, M.; Hoare, B. -N.; Vincent, S.; Guérineau, V.; Mély, Y.; Michel, B. Y.; Burger, A.

You might still get the meeting. You might still get a few questions. Because if you can’t explain your value clearly, your audience assumes there is none. But your audience isn’t evaluating you as a researcher. And when you focus on what your audience actually needs to hear, you don’t just earn attention, you earn If your pitch keeps stalling, stop editing your deck. Start refining your message.

You track the burn rate. You watch the runway shrink. You delay hires. You assume your CSO knows where you’re headed. You assume the board is aligned with milestones. You assume your cofounder sees the same finish line you do. Your CSO is not your COO. Your SAB is not your operating committee. Your cofounder is not your board.

Schild analysis is one of the few tools that tells you whether your “competitive antagonist” is actually This week, we help you tighten your interpretations and strengthen your decisions at the bench and in Quantify affinity you can defend.   Anyone who joins before the change is fully grandfathered  — your rate stays locked, and your whole team publications, events, insights, and opportunities designed to support your career, your lab, or your

GPCR Community, If the past few years have been about finding our rhythm, this year has been about refining Whether you’re an established expert or an early-career researcher, you and your lab will receive a complimentary one-year Premium Membership  when you lead a course. As we grow, we’d love to hear from you — and work with you. You can always reach me at hello@DrGPCR.org  — and yes, we read every email.

“The sooner you get your molecule in vivo, the sooner you know whether anything’s happening—and whether Kenakin reminds us: “Allostery will seek you—even if you don’t seek it.” Monthly AMAs  where you can challenge Dr. Kenakin with your own enzyme or GPCR interaction puzzles. This AMA helps you read that story faster, so you don’t just generate data—you generate direction. 🟢 40 years of expertise at your fingertips:   Explore the complete library ➤ ✳️ Want to know what’s inside

Welcome back to your weekly GPCR quest! Thank you to all participants in Dr. Terry Kenakin's educational initiative this fall! Your dedication has greatly enriched the learning experience. Get your 5-day free trial TODAY!

Enhance your GPCR research with deeper assay insights for more effective results. This Week’s GPCR Intelligence: If you want cleaner decisions, start with the system—then the ligand. Your membership gives you:   Proven   frameworks  for real-world GPCR drug discovery Flexible , on-demand Prediction, it turns out, is only powerful if you understand its limits. 🎧 Catch up while you wait: It’s built to compress your time to clarity—so you can pick better targets, stress-test hypotheses earlier

Every GPCR assay that makes it to market carries years of failures, late-night ideas, risky bets, and David Parker spent years designing rare-earth europium probes. You’ll fail 90% of the time. The fun is what you do with the other 10%. 🎯 From Launch to Legacy For Dr. It’s when you invite the community in.

This session gives you the tools to anticipate those twists before they hit your program. work in your favor? The teaser question How could you design your next lead to recruit the body’s own feedback loops in your do you need an inverse agonist to get the clinical outcome you want? Your molecule isn’t failing—your model might be too simple.

strengthen) your decisions. Terry Kenakin to elevate your science and sharpen your calls. Protect your screening funnel:  Use hemi-equilibrium readouts to flag artifacts before they inflate your We’ve got your GPCR Track, Happy Hour, and sessions mapped so you can extract maximum value. If you need to brief leadership, plan experiments, or time a move in the market or your career, Premium

If you’ve ever squinted at two curves and thought, “That looks different… I think” , you already know You need statistical methods that tell you, with confidence, whether the effect you’re seeing is real your experiment. It gives you the power to compare slopes and elevations statistically—so you can confirm whether your It’s a shift in how you approach discovery. And once you make that shift, you’ll never go back.

, potentially saving your team from costly late-stage failures. your decisions. , ensuring your candidates have the persistence needed for clinical impact Amplify your work with high-impact visibility. Submit your paper today to secure your work in Volume II ➤ Why Dr.

If you’re applying orthosteric logic to modulator-driven systems, you’re likely misreading your assays—and potentially misclassifying your leads. This lesson helps you reframe how you interpret allosteric interactions —not as simple ligand displacement If you’re still using orthosteric assumptions to interpret allosteric binding data, you're likely missing Don’t just keep up, get ahead. 🟢 40 years of expertise at your fingertips:   Explore the complete library

You can have the most brilliant minds and cutting-edge assays, but if your science isn't continuously I'll show you how to transform your drug discovery process from a series of disconnected efforts into Learn to tie your program's progress directly to your funding runway, incorporating crucial early commercial If you're ready to move beyond the articles and build these systems for your own GPCR program, let's /drgpcr/yamina-corner Or explore how we can work together: 👉 Yamina.org

GPCR Ecosystem Member, you've been with us as we've laid the groundwork for something truly special. This new learning hub is your go-to space to revisit core pharmacology concepts, master new ones, and sharpen your thinking to directly advance your drug discovery program.   Your Exclusive Premium Member Benefit:   As a thank you for your continued support of the Dr. We're excited for you to dive in.   Warmest Regards, The Dr. GPCR Team & Terry’s Desk

Your program isn’t slipping because of bad science — it’s bleeding money because your systems were broken And when you chain your highest-paid scientists to repetitive admin work, you’re not solving problems — you’re multiplying them. If you want your program to survive, you need a Blueprint for Precision. Not next quarter. Because the truth is harsh: in drug discovery, you don’t run out of science. You run out of money.

Hi GPCR Fanatics,   This week’s insights will help you avoid wasted time, poor forecasts, and stalled Your 1-minute feedback shapes what we spotlight next week. Help us help you. exclusive discount in the full newsletter   Secure Your Access Now ➤ 🗣️ “Thank you for bringing this Find your edge:  Dodge the traps that derail real drug discovery careers.  

If you’re not accounting for their limitations today, your team risks costly misinterpretations that pace of innovation in medicinal chemistry is accelerating—and if you missed this year’s ACSMEDI-EFMC Medicinal Chemistry Frontiers 2025 , you’re already behind. GPCR Premium Membership Gives You an Edge Dr. GPCR Premium gives you an edge in a fast-moving field.

Terry Kenakin to elevate your science and sharpen your decisions. Sharpen your discovery decisions ➤ Dr. This isn’t just a newsletter; it's a strategic tool for your career and your science. GPCR Course Attendee FAQ: What You Get with Dr. GPCR Premium What’s included?   GPCR Premium Membership gives you direct access to the experts and insights that can redefine your work

But what if your system just wasn't sensitive enough  to see what it was really doing? In this eye-opening module, Terry Kenakin explores a concept that could change how you interpret pharmacological It’s not just about what your molecule does —it’s also about how capable your system is at showing it If you're an emerging drug hunter, this lesson is your bridge from data confusion to predictive clarity

Imagine running a calcium assay and discovering your compound shows only weak activity. What if that result wasn’t telling you the whole story? You’ll learn why calcium signals are inherently transient—giving rise to a “hemi-equilibrium” window that can significantly distort your understanding of drug potency. If you're starting out in pharmacology, this lesson gives you the interpretive tools to ask smarter questions

Imagine you're navigating a vast terrain—not on foot, but through the shape-shifting world of GPCRs. In this exclusive Expert Drug Hunter lesson, Terry Kenakin dismantles 100 years of receptor theory and introduces you to a dynamic new framework: Molecular Dynamics. With the right lens, you’ll see why efficacy is more than signal strength: it's a fingerprint of conformational

Yamina’s Corner opens for strategic consulting, and our partner Celtarys unveils a robust TR-FRET assay Dr.GPCR Updates Terry’s Corner is Live - Pharmacology at your fingertips Terry’s Corner is now open! Elevate your drug discovery program with 45+ lessons yearly. Join Terry’s Corner Today Yamina’s Corner Is Live – Are you drowning in disorganized data? Want the full breakdown and your discount code for Terry's Corner?