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Terry’s Corner, Celtarys' Leap, and the $7B GPCR Horizon




Hello GPCR Minds,

 

This week, you'll learn all about Terry’s Pharmacology Corner, your new learning space focused on GPCR pharmacology. Whether you’re early in your career or pushing the edge of MoA design, weekly lesson help you apply key concepts like binding, signaling, and kinetics in practical, decision-shaping ways. The Corner comes will live monthly AMA sessions with Dr. Kenakin. Get curated content at your own pace.

 

Subscribe to The Kenakin Brief below to stay in the know.


Celtarys Research expands its assay tools with CELT-419 for D3 receptor studies, and Dr. Maria Majellaro shares her journey to founding Celtarys in "From Lab to Leadership". Explore her path from postdoc to platform builder.

 

Also this week: 


– Phosphorylation’s selective role in β-arrestin recruitment across class B1 GPCRs 

– GPCR mutations in cancer—drivers, passengers, or both? 

– CXCR4 oligomer disruption boosts therapeutic response in lymphoid neoplasms



Dr. GPCR Updates



Learn Pharmacology That Drives Discovery – From Dr. Terry Kenakin

 

Terry’s Corner is your space focused on GPCR pharmacology designed just for you.  Dr. Terry Kenakin brings translational clarity to complex receptor concepts.  

This is more than review, it’s readiness.

  • Learn binding, bias, kinetics, and core models—fundamentals that fuel confidence and fluency

  • Move beyond theory to apply selectivity, ADME, and early safety in real development contexts

  • Advance with nuanced lessons on allostery, residence time, and translational PK/PD

 





Fluorescent Probe CELT-419 Powers D3R Binding Assays Across Platforms

 

Celtarys Research presents CELT-419, a nanomolar-affinity fluorescent ligand optimized for D3 receptor assays in both baculovirus and live-cell systems. With strong signal stability, HTS compatibility, and broad assay versatility, CELT-419 is designed for deeper kinetic, competitive, and equilibrium binding insights.

  




The Story Behind Celtarys – From Chemistry to Company

 

How does a medicinal chemist become a biotech founder? This blog post breaks down Dr. Maria Majellaro’s path from lab research to co-founding Celtarys, as told in her recent Dr. GPCR Podcast appearance. Read how scientific need and timing drove the leap from academia to application.

 


GPCR Publication Highlights

 

  1.  Phosphorylation selectively regulates β-arrestin recruitment across glucagon family receptors, revealing that GLP-1R and GIPR rely on phosphorylation while GCGR does not. 

  2. GPCR mutations in cancer show both driver-like patterns and high redundancy, prompting a call for multiomics to distinguish signal from noise. 

  3. CXCR4 oligomerization sustains oncogenic signaling in lymphoid neoplasms, and its disruption boosts sensitivity to the apoptosis-inducing drug venetoclax.



Want the full breakdown?

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





Keep pushing the boundaries, because your work moves molecules and medicine forward. 

 

Stay curious,

 

The Dr. GPCR Team

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