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GPCR Drug Discovery at Discovery on Target 2025 — The Track You Can’t Miss If you work in drug discovery And at this year’s Discovery on Target  meeting in Boston, the GPCR Drug Discovery track will deliver I’m honored to be chairing a session  in this track — with none other than Terry Kenakin  on the speaker When we step into the GPCR track at Discovery on Target, we’re not just participating. Structure-based design  powered by cryo-EM and AI. 🔬 Inside the GPCR Track Agenda Expect deep dives

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

October 2022 Cholesterol-Dependent Dynamics of the Serotonin1A Receptor Utilizing Single Particle Tracking To explore the role of cholesterol in lateral dynamics of GPCRs, we utilized single particle tracking

We used TIRF microscopy and a statistical method to track and classify the motion of different receptor

To explore the role of cholesterol in lateral dynamics of GPCRs, we utilized single particle tracking

October 2022 Dimerization of β2-adrenergic receptor is responsible for the constitutive activity subjected to inverse agonism "Dimerization of beta 2-adrenergic receptor (β2-AR) has been observed across various physiologies. However, the function of dimeric β2-AR is still elusive. Here, we revealed that dimerization of β2-AR is responsible for the constitutive activity of β2-AR generating inverse agonism. Using a co-immunoimmobilization assay, we found that transient β2-AR dimers exist in a resting state, and the dimer was disrupted by the inverse agonists. A Gαs preferentially interacts with dimeric β2-AR, but not monomeric β2-AR, in a resting state, resulting in the production of a resting cAMP level. The formation of β2-AR dimers requires cholesterol on the plasma membrane. The cholesterol did not interfere with the agonist-induced activation of monomeric β2-AR, unlike the inverse agonists, implying that the cholesterol is a specific factor regulating the dimerization of β2-AR. Our model not only shows the function of dimeric β2-AR but also provides a molecular insight into the mechanism of the inverse agonism of β2-AR." Read more at the source #DrGPCR #GPCR #IndustryNews Subscribe to the Dr. GPCR Newsletter

Check out our new on-demand course on non-canonical GPCR behaviors and a podcast episode tracing 30 years engagement, a biased NTSR1 modulator targets pain without the need for opioids, and a real-time lipid probe tracks

In order to fast-track these advancements, an improvement in tools for their study must happen. These probes facilitate localization of receptors, tracking of their internalization and are also safer They are easier to handle and store, which also lowers outsourcing.  

CRO scopes, meticulously review assay data, flag risks early, and keep your programs relentlessly on track Systems That Drive Progress:  From assay tracking to data workflows, I design simple, scalable tools

Handling of radioligands must be done by trained users in specific facilities and using specific equipment Ease of handling is the other key difference, because fluorescent compounds do not require regulatory

Upcoming events:   Preview of Discovery on Target 2025 (Boston, Sept 24‑25), including GPCR‑Track breakout direct binding to functional sites, live-cell compatibility, and higher specificity enable real-time tracking We’ve got your GPCR Track, Happy Hour, and sessions mapped so you can extract maximum value.

future where this system is not just used for detection, but for functional screening : add ligands, track

August 2022 "Genetically encoded fluorescent biosensors allow intracellular signaling dynamics to be tracked By combining fiber photometry with FRET-based biosensors, we were able to track GPCR-dependent signaling

You’re no longer tracking the same protein species—and that changes everything. Functional assays  track another.

It began with an unmet need: how to track Gq-coupled GPCR activity without the mess of calcium flux or That opened the door to something rare in functional pharmacology: plate-based GPCR internalization tracking

We’re also tracking biased signaling in Class B GPCRs, the membrane-driven modulation of mGluR2, and

advantages enumerated previously, fluorescent ligands provide new capabilities: -            Real time tracking             High-throughput applications Bright and stable fluorescent ligands can be used in HTS, fast tracking

Breakthroughs this week:  Why Everyone’s Talking About Metabolic GPCRs; GPS for proteins: Tracking the Industry insights:  Metabolic GPCRs climbing the spotlight; new tools tracking receptor motion; obesity

donor-acceptor pairs with different emission spectra that don’t overlap, researchers can design assays that track This has been done in assays tracking IP1 and cAMP to detect biased agonism in GPCR ligands Table 1.

Upcoming events:  “Drug Discovery at Superluminal Speeds”; and Discovery on Target 2025—GPCR track you Catch Aaron’s full talk at Discovery on Target, Sept 24–25 in Boston. 🎥 Plus, join us at the GPCR Track

September 2022 "Yeast use the G-protein–coupled receptor signaling pathway to detect and track the mating

high-throughput screening Low sensitivity in detecting endogenous GPCRs With pHSense™, scientists can finally track

mediated signal transduction.[47] The 2000 Nobel Prize in Physiology or Medicine went to Eric Richard Kandel Dopamine exerts its action in the human nervous system via dopamine receptors and human trace amine-associated proteins, particularly kinases and phosphatases, that are involved in synaptic transmission[55,56] Kandel Kandel – Facts - NobelPrize.org. https://www.nobelprize.org/prizes/medicine/2000/kandel/facts/. 52.

AlphaFold accelerated discovery of psychotropic agonists targeting the trace amine-associated receptor

Retrograde trans-synaptic rabies virus tracing revealed that postsynaptic cAMP signaling is required

Terry’s Corner Why Terry’s Corner In a world where drug discovery is evolving faster than most can track

Many GPCR scientists trace their origin story back to a single unexpected spark. Not a grand plan.

If the experiment is done on live cells , tracking real-time receptor internalization becomes possible

this week’s Premium Edition: Industry insights:  Metabolic GPCRs in the spotlight; receptor motion tracking

Terry’s Corner   Why Terry’s Corner In a world where GPCR science moves faster than most teams can track