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What drives Gq vs. Gs selectivity at PTH1R? This new Nature Chemical Biology paper reveals cryo-EM structures of Gq-boun...
07/14/2025

What drives Gq vs. Gs selectivity at PTH1R? This new Nature Chemical Biology paper reveals cryo-EM structures of Gq-bound PTH1R—highlighting how N-linked glycans and ICL2 interactions stabilize receptor conformations that favor Gq coupling.

♦️ Two distinct Gq-bound conformations

♦️ Comparison with Gs-bound PTH1R

♦️ Strategic implications for biased agonist design

A critical advance for anyone working on class B1 GPCRs, bone biology, or biased signaling.

➡️ Read the paper https://buff.ly/lca0KCU

How do chemokines and GPCRs decode selectivity? A landmark Cell paper delivers the answer—mapping how conserved and vari...
07/07/2025

How do chemokines and GPCRs decode selectivity? A landmark Cell paper delivers the answer—mapping how conserved and variable sequence–structure elements govern interaction logic across 46 chemokines and 23 GPCRs. The result: a framework for designing ligands with altered receptor preferences.

♦️ Defines “public” vs. “private” binding determinants

♦️ Highlights role of structured + unstructured regions

♦️ Includes a web tool + viral chemokine engineering demo

This is a must-read for GPCR modelers, immunopharmacologists, and ligand engineers.

➡️ Read the paperhttps://buff.ly/lca0KCU

Stronger pharmacology drives smarter decisions in GPCR discovery. Terry’s Corner is now live—an on-demand learning hub l...
07/04/2025

Stronger pharmacology drives smarter decisions in GPCR discovery. Terry’s Corner is now live—an on-demand learning hub led by Dr. Terry Kenakin. Whether you’re refining assay strategy or evaluating data, these lessons give you the tools to think clearer and act faster.

♦️ 10 concise lessons + new weekly content

♦️ Short videos, crisp takeaways, and handpicked references

♦️ Built for GPCR scientists and decision-makers

Also in this week’s Dr. GPCR Weekly:

♦️ Yamina’s Corner—GPCR consulting to de-risk and accelerate your pipeline

♦️ Celtarys’ validated TR-FRET assay for CB1/CB2

♦️ Chemokine-GPCR selectivity decoded

♦️ PTH1R structures reveal Gq bias mechanisms

♦️ NMBR simulations uncover new activation pathways

♦️ Axcelead & Superluminal expand collaboration

♦️ Industry momentum: collaborations, new data, and next-gen GLP-1 strategies

Unlock deeper insight—starting now.

➡️ Read the newsletter: https://buff.ly/lca0KCU

Terry's Corner is Officially LIVE! 🎉This is your new go-to for mastering drug discovery pharmacology. No fluff, just cle...
07/02/2025

Terry's Corner is Officially LIVE! 🎉

This is your new go-to for mastering drug discovery pharmacology. No fluff, just clear, on-demand insights from Dr. Terry Kenakin.

Building core expertise? Master dose-response, binding, kinetics, and foundational models.

Driving drug discovery? Apply pharmacology to selectivity, ADME, and strategic decision-making.

An experienced drug hunter? Sharpen your edge with allosteric bias, residence time, and translational PK/PD.

Learn on-demand, apply immediately: https://buff.ly/OYnprcC

Some biotech stories start in the lab. Celtarys started with a thesis project, a new chemical strategy, and a vision to ...
07/02/2025

Some biotech stories start in the lab. Celtarys started with a thesis project, a new chemical strategy, and a vision to make fluorescence available for drug discovery. Now, they’re growing fast and partnering with Dr. GPCR to connect with the researchers who need them most.

✳️ Learn more about the partnership: https://buff.ly/7Hb37Jt

On July 1, Terry’s Corner opens with 10 pharmacology deep-dives—designed to make you rethink what you thought you knew a...
06/30/2025

On July 1, Terry’s Corner opens with 10 pharmacology deep-dives—designed to make you rethink what you thought you knew about pharmacology.

Included in the first drop:
🟢 The real role of pharmacology in discovery
🟢 Black & Leff's model of agonism—finally made clear
🟢 Binding curves, orthosteric theory, and affinity vs efficacy
🟢 Molecular dynamics and what they reveal about receptor behavior
🟢 Why Terry built this series—and how it can shape your next program

🗓️ No scheduling. No fluff. One new course drops every week.

Subscribe to The Kenakin Brief to stay in the loop.
👉 https://buff.ly/2c6dXnI

Unlock your pharmacology potential with Terry’s Corner.No fluff. Just clear, on-demand insight from Dr. Terry Kenakin—bu...
06/28/2025

Unlock your pharmacology potential with Terry’s Corner.
No fluff. Just clear, on-demand insight from Dr. Terry Kenakin—built for scientists at every level.

🟢 Building core expertise?
Learn dose-response, agonism, binding, bias, kinetics, and the models that build real confidence.

🟢 Driving drug discovery?
Apply pharmacology to selectivity, ADME, early safety, and smarter decision-making.

🟢 Already a drug hunter?
Sharpen your edge with allosteric modulation, residence time, molecular dynamics, and translational PK/PD.

Learn on-demand. Apply immediately.
Early access begins July 1 → https://buff.ly/2c6dXnI

Generic tools won’t solve tomorrow’s drug discovery challenges. That’s why Celtarys designs custom fluorescent probes fo...
06/27/2025

Generic tools won’t solve tomorrow’s drug discovery challenges. That’s why Celtarys designs custom fluorescent probes for every target, built for real pharmacology, not just convenience. With Dr. GPCR and Celtarys joining forces, expect more visibility, more precision, and more scientific impact.

🚀 Get to know our media partner: https://buff.ly/7Hb37Jt

From receptor theory to real-world assays—GPCR innovation is scaling up.Terry’s Corner is launching soon to deliver deca...
06/27/2025

From receptor theory to real-world assays—GPCR innovation is scaling up.

Terry’s Corner is launching soon to deliver decades of pharmacological expertise, while Celtarys shares powerful assay strategies and the leadership behind them.

♦️ Novo’s amycretin hits 24% weight loss; semaglutide patent opens new doors
♦️ CXCR4 nuclear signaling guides red blood cell maturation
♦️ CXCL13/CXCR5 and biased 5-HT1A are emerging pain targets

Explore this week’s GPCR breakthroughs
https://buff.ly/xkl2FtJ

GPCR pharmacology has evolved. Your training should too.Enter Terry’s Corner—a new digital learning platform where 40+ y...
06/25/2025

GPCR pharmacology has evolved. Your training should too.

Enter Terry’s Corner—a new digital learning platform where 40+ years of drug discovery meets modern pharmacology. Led by Dr. Terry Kenakin, this series breaks down complex topics including:

• Agonism & efficacy through the lens of the operational model
• Binding kinetics using real-world dose-response curve analysis
• Allosteric modulation in the context of biased signaling and molecular dynamics

Designed for scientists building GPCR-targeted drugs—not just passing exams.

👉 Early Access starts July 1st, 2025 https://buff.ly/2c6dXnI

What if β-arrestin recruitment doesn’t follow the same rules across a receptor family?A new study in the Journal of Prot...
06/24/2025

What if β-arrestin recruitment doesn’t follow the same rules across a receptor family?

A new study in the Journal of Proteome Research (Lamb et al., 2025) used mass spectrometry to map phosphorylation in GLP‑1R, GCGR, and GIPR—revealing distinct rules for β-arrestin engagement.

♦️ GLP‑1R and GIPR require phosphorylation for β-arrestin recruitment
♦️ GCGR engages β-arrestins independently of phosphorylation
♦️ Highlights receptor-specific phospho-barcodes within class B1 GPCRs

This study refines our models of biased signaling and offers a clearer path to selective drug design.

📖 Differential Role of Phosphorylation in Glucagon Family Receptor Signaling Revealed by Mass Spectrometry
Ian M. Lamb, Alex D. White, Francis S. Willard, Michael J. Chalmers, Junpeng Xiao
Journal of Proteome Research, 2025
https://buff.ly/2F0oO5c

What’s next in GPCR learning?Terry’s Corner—created by Dr. Terry Kenakin—is built to give pharmacologists real translati...
06/20/2025

What’s next in GPCR learning?
Terry’s Corner—created by Dr. Terry Kenakin—is built to give pharmacologists real translational power, not just theory.

Subscribe to The Kenakin Brief for early access and weekly updates on the platform’s launch and scientific content roadmap.

This week in Dr. GPCR Weekly:
♦️ Terry’s Corner preview: binding, bias, kinetics, PK/PD—built for drug development fluency
♦️ Learn how CELT-419 from Celtarys enables powerful probing of D3 receptor biology across assay formats
♦️ Dr. Maria Majellaro shares her journey from postdoc to biotech co-founder
♦️ GLP-1R, GIPR, and GCGR show distinct β-arrestin signaling dependencies
♦️ Not all GPCR mutations in cancer are drivers—multi-omics can help decode them
♦️ CXCR4 oligomer disruption reveals a new lever in lymphoid cancer therapy

The insights are building fast. Stay in the loop.

https://buff.ly/OiTeUXc

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