The Hidden Driver of GPCR Drug Success: Why Target Residence Time Matters More Than You Think
- Dr. GPCR News
- Aug 21
- 4 min read
Updated: 6 days ago
Hey GPCR Fans,
This week's breakthroughs are crucial for staying ahead in the rapidly evolving landscape of GPCR research and drug discovery.
Dr. Terry Kenakin's insights on target residence time can reshape how you evaluate and advance lead compounds, potentially saving your team from costly late-stage failures.
That's exactly what Dr. GPCR delivers every week: practical tools and critical intelligence to elevate your science and sharpen your decisions.
Breakthroughs this week: Novo Nordisk cuts Ozempic® cost; Nxera launches obesity pipeline; Superluminal–Lilly cardiometabolic partnership; New GPCR allosteric sites; GPCR signaling potentiation by ATP and sugars.
🔍 This Week in Dr. GPCR Premium: Sneak Peek
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Industry insights: Discover the latest strategic moves in the pharmaceutical sector, from new pipelines targeting obesity to significant collaborations in cardiometabolic disease, and gain insights into novel approaches in neurodegeneration and antibody therapeutics.
Upcoming events: Stay informed about key global conferences and symposia focusing on GPCRs, neuropharmacology, drug discovery, and biophysics, ensuring you don't miss crucial networking and learning opportunities.
Career opportunities: Explore a selection of high-level job openings in high-throughput screening, research, biologics development, clinical operations, and biostatistics within leading organizations.
Must-read publications: Stay updated on cutting-edge research, including the potentiation of GPCR signaling by ATP and sugar monophosphates and the identification of a novel allosteric site on the vasopressin V2 receptor.
Terry's Corner - Unlock the Power of Target Residence Time in Your GPCR Drug Discovery Pipeline
Gain a critical edge by understanding the in vivo efficacy drivers overlooked by traditional potency metrics.
Are your promising in vitro results failing to translate into real-world clinical success?
Dr. Terry Kenakin’s latest insights delve into target residence time, revealing why kinetic persistence often trumps binding affinity for in vivo efficacy.
Discover how factors like restricted tissue diffusion and receptor density can dramatically alter drug action, potentially unlocking the true potential of your lead compounds.
Problem Solved: Eliminate the blind spots in your drug evaluation process, moving beyond simple potency measures to understand the dynamic interactions that govern in vivo effectiveness.
Competitive Edge: Identify high-value compounds that might be missed by traditional screening methods, gaining a first-mover advantage in developing more effective therapeutics.
Threat Avoided: Prevent costly late-stage failures by incorporating kinetic modeling early in your pipeline, ensuring your candidates have the persistence needed for clinical impact.
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Dr GPCR Podcast – Decoding the Deadly Duo: Xylazine, Fentanyl, and Respiratory Depression
Understand the synergistic mechanisms driving the escalating opioid crisis and the crucial role of GPCR pharmacology.
The opioid crisis is evolving with the dangerous combination of fentanyl and the veterinary sedative xylazine.
This week’s featured podcast episode with Catherine Demery explores the distinct yet lethal mechanisms by which these drugs impair respiration.
Learn how fentanyl slows inhalation via opioid receptors, while xylazine prolongs exhalation through alpha-2 adrenergic receptors, creating a synergistic effect that drives overdose deaths.
Catherine’s research, blending GPCR signaling studies with public health data, offers critical insights into this urgent crisis.
Problem Solved: Gain a deeper understanding of the pharmacological underpinnings of opioid overdose, informing the development of more effective intervention strategies.
Competitive Edge: Stay informed on emerging public health threats and the scientific research aimed at addressing them, positioning your work at the forefront of critical biomedical challenges.
Threat Avoided: Recognize the growing prevalence and dangers of xylazine-laced opioids, enabling you to contribute to solutions and understand the broader impact on public health.
Call for Papers – GPCRs: Signal Transduction Volume II
With over 21,000 views and 7,785 downloads from Volume I, the Signal Transduction Research Topic is back. Volume II invites experts to deepen our collective understanding of GPCR pathways in health and disease.
Manuscript summary deadline: 24 September 2025.
Final submissions: 12 January 2026.
Why contribute:
Join a global, like-minded GPCR community.
Shape the next generation of cellular biochemistry research.
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