How Understanding Intracellular Drug Access Can Transform Your GPCR Drug Discovery Program
- Dr. GPCR News
- Aug 7
- 4 min read
Updated: Aug 9
Welcome back GPCR fans,
The pace of GPCR innovation is accelerating at a rate that can be difficult to keep up with. For drug discovery teams and scientists, staying ahead requires more than just reading papers—it demands access to the right frameworks and expert insights that separate the noise from the signal.
That’s exactly what Terry’s Corner delivers every week: practical tools from Dr. Terry Kenakin to elevate your science and sharpen your decisions.
Breakthroughs this week: Glucagon-like Peptide-1 Receptor (GLP-1R) Signaling; Proximity-Dependent Proteomics; Multicolored sequential resonance energy transfer.
🔍 This Week in Premium: Sneak Peek
Don't miss the key insights and opportunities that are shaping the future of GPCR research and drug discovery right now. This week's Premium content offers a curated look at what's moving the industry and scientific community forward.
Industry insights: Crinetics' Palsonify gains momentum in acromegaly, a key indicator for pipeline expansion; Septerna's chart signals upward expansion; and a look at how chronic diseases are driving growth in the global GPCR targeting market.
Upcoming events: Get details on the "neuroGPCR" symposium focusing on receptor signaling and a platform for unlocking "undruggable" targets with AI-powered hit discovery.
Career opportunities: New openings for a postdoctoral research position in GPCR biochemistry and biophysics and a research associate/scientist in in vitro pharmacology.
Must-read publications: A deep dive into proximity-dependent proteomics of adenylyl cyclase isoforms, a case for functionally Gs protein-selective GPCRs, and new methods for detecting simultaneous ligand binding.
Terry's Corner : Unlock the Power of Intracellular GPCR Drugs
For years, GPCR drug discovery has focused on targets at the cell surface. But what if the most significant opportunities lie just inside the cell membrane?
This week Dr. Terry Kenakin delivers a game-changing framework for teams grappling with the gap between in vitro potency and in vivo performance.
His latest lecture is a guide to understanding why intracellular drug access changes everything—from target residence time and rebinding kinetics to the discovery of previously untargetable sites.
Solve the in vitro/in vivo disconnect: Understand why traditional potency measurements often fail to predict clinical success and learn how intracellular kinetics can provide the missing link.
Gain a competitive edge: Learn to leverage restricted diffusion and rebinding to create drugs with longer therapeutic coverage, even with shorter systemic exposure.
Avoid missed opportunities: Discover how to identify and target cryptic intracellular allosteric sites, opening up new avenues for "failed" or under-studied GPCRs.
To stay in the know on upcoming courses and AMA session, get the complementary Kenakin Brief, the weekly newsletter delivered directly to your inbox.
Dr. GPCR Podcast : The Future of GPCR Drug Discovery with Molecular Modeling
The field of GPCR research is being transformed by the accessibility of computational tools.
In this week's Dr. GPCR Podcast, we sit down with Alessandro Nicoli, from the Technical University of Munich, to discuss his work on olfactory receptors. He shares his journey into computational chemistry and offers a compelling look at how tools like AlphaFold are providing new starting points for drug discovery.
Learn how his research aims to develop models that can distinguish between active and inactive ligands, paving the way for computational ligand discovery even where experimental data is scarce.
Harness the power of AI: Discover how breakthroughs like AlphaFold are making previously "undruggable" targets, like olfactory receptors, accessible for computational analysis.
Bridge the gap between disciplines: Get practical advice from a computational expert on how wet-lab scientists can integrate computational tools like Python and Talktorials into their work.
Learn from a pioneer: Hear how mentorship and team science are fueling innovation in the field and providing a path for the next generation of GPCR scientists.
Call for Papers: GPCRs: Signal Transduction, Volume II
Building on the success of its first volume, the research topic "GPCRs: Signal Transduction: Volume II" is now open for submissions.
This is a critical opportunity for the scientific community to come together and share new findings on how GPCRs regulate bodily functions, health, and disease. This research topic is designed to stimulate discussion and fuel the scientific direction of future GPCR research within the field of Cellular Biochemistry.
Amplify your research: Contribute to a high-impact collection of work that will shape the future of GPCR signaling studies.
Connect with experts: Join a community of like-minded field-experts dedicated to improving our collective understanding of GPCRs in human health.
Stay ahead of the curve: Showcase your latest findings on the essential role GPCRs play in disease and their function as important drug targets.
Why Dr. GPCR Premium Membership Gives You an Edge
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This isn’t just a newsletter; it's a strategic tool for your career and your science.
“The best pharmacology teacher (Dr. Kenakin) teaming up with the best GPCR community platform to help train and inspire the next generation of scientists. Also super-valuable for those of us learning how to teach pharmacology” — Dr. GPCR Course Attendee
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What’s included? The complete Weekly News digest, curated jobs, upcoming events, classified GPCR publications, exclusive on-demand expert-led courses, and member-only discounts.
Who is it for? GPCR scientists, translational pharmacologists, biotech drug discovery teams, and decision-makers who need fast, curated, career-relevant intelligence to stay ahead.
Why now? The pace of GPCR innovation is accelerating. Those acting on the right signals today will shape tomorrow’s breakthroughs—and avoid delays others won’t see coming.
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