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- Dr. GPCR Updates
Tom Sakmar, Emily Lorenzen, and Ilana Kotliar about creating a multiplex system with DUET-tagged constructs
- New Tools, Smart Signals, and The Kenakin Brief
article GPCR Publication Highlights GLP-1R/GIPR biased agonism enhances metabolic outcomes —with dual
- How Breakthroughs Happen: Eric Trinquet on Innovation, Serendipity & GPCRs
Dual control: not just brightness but fluorescence lifetime, with drastic shifts as pH drops. Tag-lite development 🧪 Mid-2010s: Rare-earth scaffold work begins 🔬 2023: pHSense probes optimized for dual It’s the product of layered collaborations—with Durham University chemist David Parker on the probe chemistry
- Enzyme Inhibition Pharmacology: The Hidden Gatekeepers of GPCR Drug Discovery
In this session, you’ll gain: ✅ A clear map of how drugs interact with enzymes before, during, and after
- The Truth About GPCR Product Launches: Years in the Making
But a pattern emerged: some scaffolds showed dual responsiveness to pH through lifetime and brightness Mini Timeline: The Road to pHSense → Initial lanthanide probe design with Durham University (chemistry ) → Discovery of pH-sensitive dual response (brightness + lifetime) → Application to GPCR models with Revnity’s partnership with Durham (chemistry) and the Institute of Functional Genomics in Montpellier
- Orthosteric vs Allosteric Interactions— and the pHSense Shift in Internalization
If your team is arguing about “potency vs. effect size vs. duration,” this is your playbook for aligning Working closely with Professor David Parker of Durham University, Trinquet’s group cracked the scaffold
- How to Design GPCR Drugs That Work in Vivo: Strategy, Tools, and Insights
A new contributor article from our friends at Celtrays Research outlines how dual-labeled fluorescent Dual-label specificity blocks promiscuous ligand confusion Lanthanide donors + d2 acceptors = high SNR
- Why Opposing Processes Matter for Your Next GPCR Drug
Dobutamine’s dual action on beta and alpha receptors, for example, invites reflex bradycardia that blunts
- GPCR Drug Discovery at Discovery on Target: Why This Track Is About More Than Receptors
GPCR and global experts at the GPCR Drug Discovery session during Discovery on Target 2025—where groundbreaking
- Integrating Fluorescent Ligands into Flow Cytometry: Enhancing GPCR Analysis Beyond Traditional Antibody Staining
Transform Flow Cytometry in GPCR Analysis GPCRs are a tough target in traditional antibody staining due
- Purpose-Driven Opioid Research: Catherine Demery’s Academic Path
The turning point came during her master’s program in pharmacogenomics.
- Allosteric Binding Demystified: Smarter GPCR Drug Discovery
A GPCR program can collapse—not because of bad science, but because brilliant teams are forced into duct
- The Hidden Driver of GPCR Drug Success: Why Target Residence Time Matters More Than You Think
Access this week’s key insight ➤ Dr GPCR Podcast – Decoding the Deadly Duo: Xylazine, Fentanyl, and Respiratory
- Why “Displacement” Misleads You: Allosteric Binding Demystified
on G protein coupling (efficacy) γ: G protein’s effect on radioligand binding (efficacy of A) β: Dual
- Maria’s Travel Blogs: ACSMEDI-EFMC Medicinal Chemistry Frontiers 2025
This joint effort by both associations is repeated every year, with 2026’s being in Dublin, Ireland. Wendy Young’s talk, during session 3 on day 2, was also incredible. Maria alongside the other panelists during Wednesday's panel discussion. Finally, during Session 9 Prof. Now back in Europe, all she can think about is next year’s date, in Dublin, where she is sure she will
- Differential binding of Δ9-tetrahydrocannabinol derivatives to type 1 cannabinoid receptors (CB1)
During that project we tested its validity as a fluorescent probe for Tag-lite® assays, where we used Figure 2.Assay Principle: TR-FRET assay using CELT-335, a dual (CB1/CB2) fluorescent ligand that serves
- Conjugation Strategies for Probe Development
It also poses some disadvantages – just like acid-amine amide coupling, some byproducts are obtained during
- Is Your GPCR Drug Discovery Program Built for Breakthroughs or Breakdowns?
better systems, but in reality, our most brilliant and expensive minds are stuck with low-impact tasks due
- The Imprecision Problem: Why Your GPCR Drug Discovery Program Is Off-Track Before It Even Starts
But because the program is run on duct tape and heroics instead of precision.
- Misread the Curve, Misjudge the Drug: Rethinking Antagonism in GPCR Pharmacology
Competitive antagonism occurs when agonist and antagonist re-equilibrate rapidly during the experiment
- Decoding Olfactory GPCRs: How AlphaFold and AI Are Changing the Game
Their structures are hard to determine experimentally due to poor expression and the volatility of odorant
- How Fast Does a Drug Work?
When does onset rate dictate therapeutic onset, and when does offset rate predict duration?
- Building Backwards: Why Top-Down Models Could Revolutionize Pain Research
Learning from COVID-19 One striking example came from his COVID-19 work during his PhD.
- Understanding Orthosteric Binding: The Key to Drug Action
Often, a low EC50 indicates high potency, but this isn't always the case due to various biological factors
- Why Sokhom Pin Never Left GPCRs, Even When Everyone Else Did
Riding the GPCR Rollercoaster Early in his career at DuPont and BMS, GPCRs were red hot.
- Pharmacology Isn't What You Think—It's So Much More
Ever wondered why a drug behaves like a miracle in one tissue and a dud in another?
- The Chemistry of Confidence: Aha Moments That Shape Scientific Careers
Getting accepted into a PhD program during a personally difficult time.
- From Multiplex to Models: Scaling Up GPCR Discovery in the Post-Silo Era
Building for the Future The Sakmar lab built a system to meet that need: Dual-epitope tagged constructs
- From One to Many: How a GPCR Curiosity Became a Field-Wide Toolkit
What emerged was a dual-tagged GPCR library (DUET constructs), now publicly available via Addgene ,
- Inside Out: Mapping GPCRs from Membrane Codes to Market Moves
From dual-epitope tagging to scalable multiplex assays, this conversation dives deep into the tools now






























