Allostery isn’t just an advanced concept—it’s essential to understanding efficacy, ligand bias, and receptor As the GPCR field surges forward—from ligand bias to signaling diversity—the guest editors Dr. Why you need to be there: Learn how kinetic nuance shapes ligand design.   Access peer insights on allosteric modulators and biased ligands. GPCR Podcast Listener Why Dr.

Breakthroughs this week: Glucagon-like Peptide-1 Receptor (GLP-1R) Signaling; Proximity-Dependent Proteomics But what if the most significant opportunities lie just inside the cell membrane? This week Dr. Learn how his research aims to develop models that can distinguish between active and inactive ligands , paving the way for computational ligand discovery even where experimental data is scarce. " targets, like olfactory receptors, accessible for computational analysis.

The Early Days: Molecules and Mentors Alessandro began his academic life studying pharmaceutical chemistry every day the results, I was getting in love with the topic and decided—yeah, I want to do this in my life With hundreds of subtypes and limited ligand data, olfactory GPCRs represent a high-risk, high-reward

This approach reflects his focus on developing models that behave  like patients before molecular exploration hypothesis, Serafini’s team noticed that hamsters infected with SARS-CoV-2 exhibited persistent pain-like This patient-centric and behavior-first approach uncovered robust gene expression signatures  linked He also integrates concepts like sex differences , epigenetic inheritance , and neuroimmune crosstalk

. 👉 Dive into Terry’s Vault and see agonism like never before Unlock "Agonism & Sensitivity" now

Through real-world examples (like 5-HT2A and CCR5 agonists), Terry shows how slow-onset agonists can Because when true pharmacological profiling is essential—like detecting partial or inverse agonism—calcium

into clinical forecasts The 4 types of pharmacologic models (and when to use each) The truth about linear How the Mass Action Law underpins nearly every model Future of Receptor Theory: Linkage vs.

Serafini described his connection to GPCRs as tangential but inevitable: "I feel like I never was particularly highlighted that in modern pain drug development, the field has remained too focused on ion channels like NAV1.8 , despite these targets falling short clinically: “The downstream cascade is probably a little bit weaker than if you were hitting a GPCR... and honestly, like with the trials, they were not really The real power may lie in how they’re regulated. Dr.

Terry Kenakin’s featured talk on “The Kinetics of Allostery” offers a rare live glimpse into advanced Identify emerging targets:  Allosteric modulators, biased ligands, and kinetic frameworks will dominate

After years of living with unresolved pain following surgery for a pilonidal cyst, Alex was left without This is a story about how chronic pain doesn't just shape lives — it reshapes careers. The Value of Lived Experience in Science What makes Serafini’s trajectory so compelling isn’t just his His interest in model development, in capturing the lived human experience through preclinical systems He’s focused on RGS proteins , pain comorbidities  like addiction and depression, and pushing for more

By considering factors like the Langmuir adsorption isotherm and binding curves, researchers can better

These ongoing conversations keep me on the front lines, sharpening my understanding of the common bottlenecks

recovering from a stall, I’ll help you move faster—with fewer blind spots, tighter execution, and a clear line

But Sokhom Pin stayed loyal to GPCRs , even when big pharma turned its gaze to other targets like kinases High-throughput screening for receptor ligands was booming, and Sokhom was at the center of it.

just credentials He designed lab workflows that encouraged curiosity without burnout He supported work-life In a field like GPCR research (where data complexity and failure rates are high), scientific rigor thrives Alkermes didn’t just improve drug screening outcomes, it redefined what great leadership in biotech looks like

As a lab technician at Johns Hopkins, he was fascinated by science but also grounded in real-life responsibilities Takeaway If you’re navigating work, life, and scientific ambition, Sokhom Pin proves it’s possible to

Welcome Back, Discovery Drivers   Terry’s Corner is live, on-demand pharmacology built for drug discovery Dr.GPCR Updates Terry’s Corner is Live - Pharmacology at your fingertips Terry’s Corner is now open! Join Terry’s Corner Today Yamina’s Corner Is Live – Are you drowning in disorganized data? GPCR partner Celtarys Research has validated a TR-FRET assay for cannabinoid receptor ligands using their Distinct Ligand Activation in NMBR Simulations show how two ligands differently activate class A GPCR

Eli Lilly’s next moves with Orforglipron and its amylin analog are highly anticipated.   Plus, Celtarys explores ligand selection for better assays, and co-founder Dr. Maria Majellaro shares her story of innovation and listening-driven science.   Sign Up for The Kenakin Brief Fluorescent Ligands vs. Radioligands – Assay Smarter Celtarys explores how fluorescent ligands enable safer, high-throughput

Ever wondered why a drug behaves like a miracle in one tissue and a dud in another?

What happens between identifying a target and delivering a life-saving treatment? In this foundational-level  lesson, Terry unpacks the real-life process behind discovering new drugs,

Maria Majellaro makes it clear that Celtarys isn’t just a ligand provider. Maria Majellaro Celtarys specializes in the custom development of fluorescent ligands  using a modular Their method allows researchers to explore different linker positions, tailor activity (agonist or antagonist Maria emphasizes the importance of genuinely listening to researchers: understanding the biological question discovery workflow on the company page . _______________ Keyword Cloud:   GPCR data platform , fluorescent ligands

re early in your career or pushing the edge of MoA design, weekly lesson help you apply key concepts like The Corner comes will live monthly AMA sessions with Dr. Kenakin. Binding Assays Across Platforms   Celtarys Research presents CELT-419, a nanomolar-affinity fluorescent ligand optimized for D3 receptor assays in both baculovirus and live-cell systems. GPCR mutations in cancer   show both driver-like patterns and high redundancy, prompting a call for multiomics

Watch Episode 168 Success in science is rarely linear. Maria Majellaro Now, she leads a team of talented chemists at Celtarys, developing fluorescent ligands company page . _______________ Keyword Cloud:   GPCR scientist network , career development , fluorescent ligands

Maria worked with had developed a technology that allowed for flexible, fast synthesis of fluorescent ligands

readouts: proximity, immuno assays, pulldowns Validated antibodies + digital search platform Entire library  (e.g., 14-3-3) Heterodimerization Endogenous vs. overexpressed systems Orphan GPCR deorphanization Ligand students and visiting scientists are already expanding this work, bringing in computational layers  like Listen to the complete episode to learn more. _________________ Keyword Cloud : GPCR scientist network

GPCRs in Disease Sakmar highlights how endothelial cells, which express a wide array of GPCRs, are likely The Tools to Detect Them Using the multiplexed GPCR library and Luminex assay , researchers can now: sees a future where this system is not just used for detection, but for functional screening : add ligands

This collaboration aims to amplify the visibility and adoption of Celtarys’ cutting-edge fluorescent ligand Celtarys Research develops high-quality, fluorescently labeled ligands and innovative chemical biology These tools enable high-resolution binding studies, kinetic analysis, and live-cell imaging, empowering “We’re thrilled to partner with Celtarys and introduce their high-performance fluorescent ligands to binding in live cells, and design better experiments, core to advancing GPCR-targeted discovery.”

trajectory in motion, culminating in a scalable, multiplexed platform to investigate GPCR-RAMP biology  like What emerged was a dual-tagged GPCR library  (DUET constructs), now publicly available via Addgene ,

arrestin engagement, a biased NTSR1 modulator targets pain without the need for opioids, and a real-time lipid Terry Kenakin, these five modules reveal how location bias, intracellular signaling, and ligand kinetics

Moments like these helped him own his identity as a scientist.