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The metrics shift: k_inact  (rate of inactivation) replaces static Ki values. k_inact/KI  becomes the

Why This Matters: IP-One helped set a new gold standard for functional GPCR assays—shifting how compounds Dual control: not just brightness but fluorescence lifetime, with drastic shifts as pH drops.

This week —NIH’s new GPCR biosensor push, a leadership shift at Septerna, and a bold thesis on stabilizing You’ll explore how catalytic control, allosteric shifts, and CYP450 behavior rewrite the rules of pharmacology

That same shift in mindset (seeing enzymes as predictable, targetable, quantifiable systems ) is exactly Their broad substrate tolerance shields us from xenobiotics.

Inside Premium:  Key FDA moves reshaping GPCR pipelines, shifting obesity and CNS strategies, and global to explore how computational modeling is evolving from explanation to real prediction — and why that shift

By modulating receptor expression or sensitivity, we can shift the “lens” through which drug activity

. ✅ Insight into Consequences:  How binding sites determine receptor state shifts, signaling outcomes Allosteric sites operate differently: ligands bind elsewhere, transmit energy changes, and shift the This has immediate implications for interpreting EC50 shifts, partial agonism, and assay readouts—especially orthosterically, allosterically, or with mixed mechanisms—and why that matters for interpreting EC₅₀ shifts

Some can make a mediocre drug shine. Get a sense of why inverse agonists may be necessary to truly shift the physiological balance.

Instead of clean monophasic curves, you’ll see biphasic signatures or sequential shifts—first cholinesterase It’s a shift in how expert drug hunters see pharmacology.

A compound shifts the curve. It elevates the baseline. But what does that really mean? Take the example Terry highlights: an agonist curve with a rightward shift and elevated baseline. The shift continues linearly. Allosteric? The shift plateaus once the allosteric site saturates. compound produced four completely different assay signatures depending on the system: Sometimes it shifted It’s a shift in how you approach discovery.

Superluminal is building systems that learn from receptor movement, conformational shifts, and complex emphasizes that building a startup is not simply a continuation of research — it requires a mindset shift

But something shifted.

While writing a literature review on opioid and alcohol addiction susceptibility, something shifted.

You’ll learn how to recognize these shifts using vivid analogies (like Bruce Wayne vs. model binding with cooperativity factors (α, β, γ, σ) using the Hall allosteric cube The Allosteric Shift It redefines how we interpret radioligand curves , shifts in signal, and the meaning of “inhibition.” Kenakin shows how even small cooperativity values (like α = 0.1) cap the shift in signal .

extended fluorescence duration, enable delayed emission readings, have narrow bands and high stokes shift

been used to study GPCRs for decades, but with the advances in the fluorescence field, assays have shifted

For example, some assays benefit from using a more red-shifted fluorescent label or a combination of

Systems for GPCR Drug Discovery The only way out for GPCR drug discovery programs isn’t more people or shinier

Kenakin’s latest lecture delivers a paradigm shift for pharmacologists working on drugs where in vitro

Why Misreading Antagonism Delays GPCR Drug Discovery If a dose-response curve shifts to the right, you DR curves shift to the right with no loss of maximal effect. One shifts neatly to the right without dropping the maximum.

—Alessandro Nicoli A New Era of GPCR Research AlphaFold didn’t just fill a gap—it shifted the focus of

Imagine you're navigating a vast terrain—not on foot, but through the shape-shifting world of GPCRs.

It’s about a dynamic dance of chemical forces, equilibrium shifts, and molecular decisions that determine

I know how to ask the right scientific questions—and when to shift from analysis to execution.

But then came the industry shift. “Companies started shutting down neuroscience and GPCR programs.

some agonists succeed in sensitive tissues but fail elsewhere—and how this knowledge can dramatically shift

GPCR-targeted drugs fail—not because of poor chemistry, but because we’ve misunderstood how these shape-shifting

“The first time I wore my lucky cactus shirt to a major meeting... and it led to a game-changing collaboration

Sakmar reflects on a generational shift in training.

Why It Matters This isn’t just a dataset, it’s a shift in how GPCR biology is approached : Study known