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These results support the use of fluorescence-based screening methods as a reliable alternative to classical

Her findings highlight how fentanyl suppresses inhalation while xylazine prolongs exhalation, creating than medicine can adapt, Catherine’s work shows why overdose research must evolve alongside the drug supply That surge mirrors what’s happening nationally. The insight is simple but urgent: the drug supply evolves faster than medicine.   And the illicit supply is moving faster than clinical medicine can adjust.

When a PAM increases radioligand binding but suppresses functional response, it’s not broken pharmacology—it Suddenly, the agonist works . Terry Kenakin An always-growing library of on-demand pharmacology insights The ability to vote on or suggest Subscribe to The Kenakin Brief today ➤ #AllostericPharmacology #GPCR #BindingVsFunction #ReceptorPharmacology

On the other hand, fluorescent ligands have a superior safety and environmental profile.

Moore, was most definitely a success. Now back in Europe, all she can think about is next year’s date, in Dublin, where she is sure she will

CELT-335 was successfully used in assays to determine the pharmacological properties of Δ9-tetrahydrocannabinol When this happens the proximity between donor and acceptor is sufficient for a transmission of energy

New scaffolds modulating the CBRs in both the orthosteric and allosteric sites have been developed, supported of the series developed by Pfizer, including CP5594, gave rise to a new class of abused psychoactive substances GPCRs are not suitable for antibody use due to steric hindrance and reverse binding, thus, other strategies Among them, we have chosen the SNAP-tag, a suicide enzyme technology. Cell-Surface Protein-Protein Interaction Analysis with Time-Resolved FRET and Snap-Tag Technologies:

the minimal chemical modifications in the original ligand, high sensitivity and their extensive and successful (3H) labeled ligands are usually chemically identical to the original, because tritium will usually substitute and more accessible alternative. -            Quantitative cell binding studies : Radioligands have superior

Introduction Dopamine receptors are G-protein-coupled receptors (GPCRs), which have 5 subtypes -D1-5. The estimated Z’ of the assay is 0.71, which is sufficient for HTS standards. Figure 3.   No substantial differences were found between them and the reporter. Figure 4.     These results indicate that CELT-419 is suitable for live-cell assay with automated microscopy. Evaluation of Fluorophores for Optimal Performance in Localization-Based Super-Resolution Imaging.

O-acylisourea rearranging intramolecularly into the N-acylurea.[ 2]     NHS ester amide coupling  is the most suited This property comes from the wide chemical space this reaction can access – we can substitute one reagent Semiquantitative Study of the EDC/NHS Activation of Acid Terminal Groups at Modified Porous Silicon Surfaces Chapter Three - Bioconjugated Materials in the Development of Subunit Vaccines.

Tackling the GPCR Imprecision Problem: Strategic Planning for Sustainable Progress in Complex Systems demands intentional planning and a systematic approach, ensuring every step forward is strategic and sustainable detail, operational process, and strategic decision aligns to create a seamless, predictable pathway to success operational strategy , emphasizing that precision is a continuous, intentional journey towards predictable success biotechs, VCs, and CROs to implement the framework that ensures every step forward is strategic and sustainable

We're launching with 10 on-demand lessons , each featuring:   A short, focused video A concise written summary Your Exclusive Premium Member Benefit:   As a thank you for your continued support of the Dr.

Surely more hands will move the needle. If you want your program to survive, you need a Blueprint for Precision. Not next quarter.

makes a drug “effective,” arguing that kinetic persistence (not binding affinity) determines real-world success But as Kenakin shows, t½ is a surface metric —a combination of clearance and volume of distribution. that explains results in animal models, informs clinical translation, and helps teams avoid late-stage surprises Subscribe to The Kenakin Brief today ➤ #TargetResidenceTime #DrugBindingKinetics #PKPDdissociation #ReceptorPharmacology

Watch Episode 171 Mentoring in science is more than supervising—it’s about shaping the next generation

Terry’s Corner takes you beyond curve shapes into the kinetic and mechanistic realities that separate surface-level transform your program from a series of disconnected efforts into a predictable, de-risked pathway to success Build predictable success:  Use a repeatable improvement framework to turn operational chaos into precision Solve the problem of information overload by getting a curated summary of the key talks and discussions

Beyond the Curve: Questions This Lesson Helps You Answer This lesson pushes you to go deeper than surface-level Why is competitive antagonism  considered reversible and surmountable, while non-competitive antagonism Each subscription includes: Weekly deep dives from Dr. Why now:  GPCR research is accelerating—and the projects that succeed will be those built on clear, accurate Subscribe to The Kenakin Brief today  ➤   #GPCRantagonism #CompetitiveAntagonists #NonCompetitiveAntagonists

But that model is no longer sufficient. Subscribers gain access to: Weekly lessons by Dr.

assays   Why Intracellular GPCR Drugs Change the Game For decades, drug design has treated GPCRs as surface And while that strategy has yielded enormous success, it ignores a powerful reality: the cytosol is a He also reviews key scaffold properties that determine success, offering practical tips for design teams GPCRs Aren’t Just Surface Receptors Anymore From β2-adrenoreceptors to CCRs and dopamine receptors, multiple Subscribe to The Kenakin Brief today  ➤ #GPCRs #IntracellularDrugs #DiffusionBarriers #DrugResidenceTime

Kenakin’s latest   lecture delivers exclusive, real-world insight designed to equip you to move beyond surface-level framework for understanding when a drug’s rate of binding onset and offset matter most for in vivo success well-informed decisions that move promising candidates forward while de-prioritizing those unlikely to succeed Your Pipeline Many workflows still operate on the assumption that equilibrium potency (Kd) alone is sufficient Missteps at this level can delay optimization, generate unnecessary SAR work, or cause your team to miss subtle

. 🔍 Quick Wins This Week 🔹 Tell us what matters → News Survey Your 1-minute feedback shapes what GPCR Podcast - Surviving Discovery’s Gauntlet Dr. Sokhom Pin delivers brutally honest insights.  

Subtle misinterpretation can quietly derail projects, slow timelines, and waste scarce resources. startup environments Read Maria Majellaro's Full Recap ➤ Lab Leadership Without Ego: A Model for R&D Success pharmacology group from scratch—not just a lab, but a culture that encouraged curiosity, empowered people, and supported for attitude and team fit—not just credentials Design workflows that enable curiosity-driven research Support

This Week in Premium: Sneak Peek Industry insights:  Strategic biotech alliances (Chemspace/Enamine, Superluminal As the GPCR field surges forward—from ligand bias to signaling diversity—the guest editors Dr. Your work belongs in the core conversation—not buried in supplementary files. Volume II isn’t about repetition—it’s about redefining signal transduction. 📝 Manuscript summary deadline : 23 Sept 2025 📄 Submission deadline: 11 Jan 2026 Submit to Volume II ➤ Discovery On Target: Where the

Power of Intracellular GPCR Drugs For years, GPCR drug discovery has focused on targets at the cell surface in vivo disconnect:  Understand why traditional potency measurements often fail to predict clinical success your computational toolkit ➤ Call for Papers: GPCRs: Signal Transduction, Volume II Building on the success Also super-valuable for those of us learning how to teach pharmacology” — Dr. To succeed, you need to move beyond standard approaches and adopt the frameworks that are driving real

Suddenly, chemistry wasn’t just synthetic—it was strategic. With hundreds of subtypes and limited ligand data, olfactory GPCRs represent a high-risk, high-reward

These findings suggest a path forward that isn’t about blocking a single receptor but about rewiring weaker than if you were hitting a GPCR... and honestly, like with the trials, they were not really that sufficiently And in itself, that's kind of a suggestion.” Serafini’s work on RGS proteins suggests a quieter, but no less powerful, frontier in the fight against

designed to keep you ahead without noise or delays: Industry insights:  Structure-Based Drug Design Summit Rethink translational success:  How post-COVID insights and unconventional decision-making shaped Serafini

After years of living with unresolved pain following surgery for a pilonidal cyst, Alex was left without

Implications for Drug Development As drug developers, understanding these nuances can significantly impact the success

Systems That Drive Progress:  From assay tracking to data workflows, I design simple, scalable tools that surface