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August 2022 A new Kunitz-type snake toxin family associated with an original mode of interaction with the vasopressin 2 receptor "Abstract Background and purpose: Venomous animals express numerous Kunitz-type We aimed to exploit other mamba venoms to enlarge the V2R-Kunitz peptide family and gain insight into Sequence comparison between active and non-active V2R Kunitz peptides highlighted five positions, among Conclusions and implications: A new function and mode of action is associated with the Kunitz peptides

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 Here’s who we've talked to so far: 🎥 Check out the interview with Dr. When we step into the GPCR track at Discovery on Target, we’re not just participating.

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

September 2022 Lack of Oestrogen Receptor Expression in Breast Cancer Cells Does Not Correlate with Kisspeptin

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

April 2022 John Streicher talks about his work on terpenes found in cannabis as these may be a novel

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

Tackling the GPCR Imprecision Problem: Strategic Planning for Sustainable Progress in Complex Systems 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 . Every time a problem arises, we trace it back to its root cause, implementing changes that prevent its Part 3: The Financial Friction : Explore how a lack of precise alignment between GPCR scientific milestones

Welcome back to your weekly GPCR quest! Financing Deal of the Year at the Citeline Japan Awards 2024 GPCR therapies: Eight promising biotechs hacking Scientific Advisory Board GLP-1s like Ozempic are among the most important drug breakthroughs ever Goldman-backed

through a suggestion from one of my colleagues to join this select group, which was getting together to talk The excitement I felt when I first attended back in Boston is the same one I feel now that I am the organizer What is your favorite taco? What mariachi song are you most likely to shout along to at 3 AM? AB: Favorite Taco: Taco de suadero (pronounced swa-day-ro), fatty, with meat caramelized in its own fat Note that Taco al Pastor is a staple among Mexico City’s delicious tacos.

The lack of transparency surrounding its operations and usage constraints restricts extensive academic Looking ahead, AI offers significant advantages in drug development, such as the ability to tackle complex

This is where seasoned drug hunters separate themselves from the pack—not just knowing the kinetics , Kenakin  will get released next month, featuring real questions from discovery scientists tackling enzyme

Terry Kenakin will conduct two back-to-back courses this fall. The two back-to-back courses are new and specially tailored to the Dr. Mechanism of the GPR183 Receptor GPCR Binders, Drugs, and more Target-based discovery of antagonists of the tick

Kotliar sums it up best: “We went from one receptor to many… and now, from many, we can go back to one

We will be back next week with our regular weekly GPCR news digest.

Welcome back GPCR lovers, In pharmacology, the wrong interpretation of antagonist behavior can derail We’re also tracking major pipeline clearouts and the competitive landscape for oral GLP-1 drugs. protein coupled receptor signaling in its physiological cellular context” symposium and our featured talk Yamina’s Corner tackles the critical disconnect between brilliant science and operational strategy, revealing Solve the problem of information overload by getting a curated summary of the key talks and discussions

Warm greetings and a resounding welcome back to our GPCR Weekly Newsletter, rejuvenated after the festive GPR84 and insights into biological control Larixol is not an inhibitor of Gαi containing G proteins and lacks Advance Novel Gene Therapies GPCR Events, Meetings, and Webinars January 16 - 19, 2024 | 23rd Annual PEP Talk

put forward to target CKRs especially in cancer, nevertheless, targeting this system is a challenging task binds to CCR1, CCR3 and CCR5, and induces different patterns of receptor recycling where CCR5 recycles back to the cell surface (Mack et al. 1998), CCR3 is partially restored to the cell surface and partially

engagement, a biased NTSR1 modulator targets pain without the need for opioids, and a real-time lipid probe tracks Access the Course Hacking GPCRs: A Toolkit for Systems Biology – New Podcast Episode In Episode 167,

tools available to study the contribution of PKC isozymes have considerable limitations, including a lack Moreover, since pharmacological tools to study PKC isozymes generally lack specificity and/or potency

🔹 Spot the opportunity → Why Catalio is betting big when others pull back Amid biotech slowdowns

Building a Career from the Inside Out Now back in med school, Serafini aims to follow the physician-scientist "When you talk to patients that have an unmet need, you learn things that no one is thinking about in

More accurate hypotheses, faster ligand discovery, and new strategies to tackle one of biology’s most

GPCR Podcast is back this week with a brand new episode. Our guest is none other than Dr.

GPCR Virtual Cafe is back! Our first guest speaker is none other than Dr. Ben Myers!

You can already explore the platform and subscribe to The Kenakin Brief—our new newsletter packed with

Kenakin will be back with two back-to-back classes.

May 2022 "Seoul, South Korea, 28 April 2022 – GPCR therapeutics, Inc., a venture-backed clinical stage