How Advanced GPCR Kinetics Sharpen Decision Making (and Save You Time)
- Dr. GPCR News
- Sep 18
- 4 min read
Hi GPCR Community,
If equilibrium curves are your comfort zone, this week’s feature will challenge (and strengthen) your decisions.
We’re zeroing in on kinetic tools that reveal what steady-state data can’t—so you can vet leads faster, avoid false positives, and move with confidence.
That’s precisely what Terry’s Corner delivers each week: practical frameworks from Dr. Terry Kenakin to elevate your science and sharpen your calls.
Breakthroughs this week: Septerna begins first-in-human trial of SEP-631 for CSU; Maxion’s KnotBody® platform; a new angle on RGS protein modulation.
🔍 This Week in Dr. GPCR Premium: Sneak Peek
Here’s a fast, high-level preview of what Premium Members are unpacking this week. It’s a curated lens—just enough signal to guide your week, with the full depth available inside.
Industry insights: Orforglipron’s trajectory is redefining weight-management and diabetes markets—implications for GPCR-linked pathways and competitive positioning.
Upcoming events: Preview of Discovery on Target 2025 (Boston, Sept 24‑25), including GPCR‑Track breakout sessions; panel opportunities to engage with biophysics and structural biology leaders.
Career opportunities: Snapshot of roles spanning PhD entry points to senior translational pharmacology—Protein Expression, Drug Discovery Scientist, and Staff Scientist in Molecular Pharmacology—curated with notes on fit, skill spikes, and timelines.
Must-read publications: From on stabilizing RGS2 via modulating its degradation (versus direct inhibition); selectivity frameworks for β₂ vs β₁ adrenergic receptors tp structural insights into cholesterol interactions in the active conformation of GLP‑1 receptor
Terry's Corner – Advanced Applications of GPCR Kinetics for Real-World Decision Making
Equilibrium looks tidy. But kinetics tells the truth.
This week, you will learn how to confirm equilibrium the right way, detect time-dependent occupancy and complex activity, leverage hemi-equilibrium calcium assays, recognize fractal potency, and surface liabilities early—before they cost you cycles and credibility.
These are the pattern-recognition tools that convert uncertainty into decisions you can defend at a project review.
Avoid expensive mirages: Spot when “good” equilibrium curves mask time-dependent binding that will fail in translational settings.
Protect your screening funnel: Use hemi-equilibrium readouts to flag artifacts before they inflate your SAR.
Out-decide your competition: Apply fractal potency insights to prioritize leads that stay robust across conditions.
Premium Members get a 50%+ discount when they join Terry’s Corner.
🚨 Live AMA with Dr. Kenakin is today, September 18th, 12-1 pm EST in Terry’s Corner. Corner members get to rewatch the recording
Celtarys Research – Flow Cytometry Reimagined: Fluorescent Ligands vs Antibodies for Live‑Cell GPCR Studies
Traditional antibody staining for GPCRs has well‑known limitations—fixation artifacts, epitope masking, low expression, conformation changes.
Fluorescent small-molecule ligands flip the script: direct binding to functional sites, live-cell compatibility, and higher specificity enable real-time tracking of interactions, internalization, and biased signaling—without fixation or permeabilization.
Learn how to choose fluorophores (brightness, stability, spectra), reduce background (far-red/near-IR), and match channels to your cytometer for clean, multiparametric data.
Eliminate fix/perm distortions: Preserve receptor conformation and downstream signaling integrity.
Get functional—not just presence—readouts: Quantify affinity and kinetics where it matters.
Scale confidently: Use bright, stable ligands for HTS and bias profiling.
Discovery on Target 2025 Speaker Spotlight: Solubilization, Orphans & Lipid Systems
In a conversation with Alison Heick Varghese and Kris Borzilleri (Pfizer), we dig into detergent-free, lipid-mimic systems for reliable GPCR screening; orphan GPCR strategies; and advances across nanodiscs, peptidiscs, SMALPs, SPR, ITC—plus how construct design and solubilization choices shape success.
In Boston, Sept 24–25? We’ve got your GPCR Track, Happy Hour, and sessions mapped so you can extract maximum value.
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