Understanding Enzyme Inhibition In GPCR Discovery Programs

Dr. GPCR News
Oct 16
4 min read

Enhancing scientific exploration by concentrating on understanding inhibition to advance GPCR drug discovery

This Week’s GPCR Intelligence:

Every drug you design will meet an enzyme before it meets its receptor. If you want your molecules to survive first contact with biology, enzyme inhibition must be part of your core playbook.

This week’s feature breaks down exactly how to think about inhibitors with rigor and speed, so you can make better decisions earlier in the pipeline.

Breakthroughs this week: Potentiation of GPCR signaling by ATP and sugar monophosphates; Pharmacology 2025; Nxera Pharma earns $10m milestone from AbbVie neurological deal.

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This week—NIH’s new GPCR biosensor push, a leadership shift at Septerna, and a bold thesis on stabilizing mutated GPCRs.

Plus: top tracks to watch at GPCR Forum 2025, fresh postdoc openings at the ADME/signaling interface, and concise reads on β-agonists, phospho-barcodes, and GPCR allostery.

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Terry's Corner – How Enzyme Inhibition Shapes Every Discovery Program

Every molecule meets an enzyme before it ever meets its receptor. Whether you’re designing a ligand, optimizing ADME, or predicting PK, enzyme inhibition defines what survives to make an impact.

This week’s Terry’s Corner reframes inhibition not as background theory—but as a design lens for smarter discovery. You’ll explore how catalytic control, allosteric shifts, and CYP450 behavior rewrite the rules of pharmacology.

Mastering inhibition isn’t just about avoiding drug–drug interactions. It’s about turning enzymes from barriers into a strategy.

You’ll discover:

How four inhibition modes (competitive, noncompetitive, mixed, uncompetitive) dictate potency, efficacy, and safety.

Why CYP450 allostery can make or break translation from bench to bedside.

When “inhibition” becomes activation—and how that insight fuels next-gen therapeutic design.

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The Innovation Trap: Why Playing It Safe Can Kill Breakthroughs

Revvity's Dr. Eric Trinquet, the scientist behind IP-One, Tag-lite, and now pHSense, challenges conventional scientific thinking in this candid post.

He argues that early-career researchers often fall into the trap of over-rationalizing too soon—missing out on the unexpected twists that lead to real innovation.

From failing fast to embracing serendipity, Eric shares the mindset (and messy origin stories) that shaped tools now used across biotech and academia.

Whether you’re building assays or a scientific career, this is a must-read on why risk, surprise, and strategy belong together.

Read the Feature ➤

Summer Days: Appetite, Suntans, and GPCR Micro-Domains

Two recent papers connect ciliary signaling, opsins, and melanocortin receptors to behaviors and skin biology. This spotlight from Montana Molecular dives into how OPN3’s modulation of MCR4 in appetite circuits and MCR1 in melanocytes highlights the power of localized cAMP and ion channel coupling to reshape physiology.

If you care about compartmentalized signaling and native-state biology, this is a sharp, readable tour.

Zoom into the cilium. Why micro-domains change what “global” signaling can and can’t explain.

Target specificity, not just potency. Localized cAMP and channel coupling as levers for phenotype.

New tools, new questions. Biosensors make once-invisible dynamics assayable at scale.

Read the roundup ➤

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