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GPCR News 

Post: Blog2_Post

New Tools, Smart Signals, and The Kenakin Brief



Hello GPCR Trailblazers,


This week, we’re spotlighting Celtarys Research, our newest partner, featured in a blog and podcast with CSO Dr. Maria Majellaro, highlighting their fluorescent ligand tools for live-cell GPCR assays.

 

After 40+ years and 250 publications, Dr. Terry Kenakin is launching a new learning space with video courses, AMAs, and practical insights. Get a sneak peek and sign up for The Kenakin Brief—his free weekly newsletter.

 

On the industry side, Novo Nordisk, Septerna, and Deep Apple advance billion-dollar GPCR programs, while Eli Lilly and Nxera move forward in metabolic disease.

 

📚 This week’s paper highlights:

  • GLP-1R/GIPR biased agonism enhances metabolic outcomes

  • Ghrelin receptor flips D2 signaling without a ligand

  • MOR-PAM shows G protein-selective bias

 

The insights are ready. The time you’ll save is yours. Terry’s Corner is coming soon.



Dr. GPCR Updates


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Terry’s Corner Is Coming – Get Early Access and Updates 

 

Terry’s Corner is launching soon with monthly courses, AMAs, and real-world pharmacology from Dr. Terry Kenakin. You can already explore the platform and subscribe to The Kenakin Brief—our new newsletter packed with sneak peeks, insights, and launch news straight to your inbox.

 




From Chemistry Lab to GPCR Partner – New Podcast with Celtarys

Dr. Maria Majellaro of Celtarys shares how her team translates medicinal chemistry into practical GPCR assay tools—and how their new partnership with Dr. GPCR will help researchers move faster with custom fluorescent ligands, translational insight, and tool-enabled discovery.



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Introducing Celtarys - Probe Development via Conjugation Strategies

 

Celtarys Research's first article provides a detailed examination of conjugation strategies to develop high-performance fluorescent probes. It emphasizes scaffold selection, linker optimization, and assay compatibility to enhance target binding and signal fidelity in GPCR applications.

  



GPCR Publication Highlights

 

  1. GLP-1R/GIPR biased agonism enhances metabolic outcomes—with dual targeting showing synergistic glucose and weight benefits.

 

  1. Constitutive ghrelin receptor activity, not dimerization or ligand binding—reverses dopamine D2 signaling in a physiologically critical circuit.

     

  2. A MOR-positive allosteric modulator (BMS-986122) selectively enhances opioid signaling through specific Gα subtypes, revealing new paths to safer analgesia.



Want the full breakdown?

Explore this week’s research, tools, and biotech insights in one place.



The insights are ready. The time you’ll save is yours. Terry’s Corner is coming soon.

Stay curious,

The Dr. GPCR Team

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