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interactome of GPCRs with receptor activity-modifying proteins Nicholas Kapolka , Geoffrey Taghon , and Daniel Isom  for their research on Advances in yeast synthetic biology for human GPCR biology and pharmacology

Weekly Highlights: Congrats to: Daniel Matúš , Simone Prömel , et al., for their work on The N terminus-only

Kenakin’s Emerging Drug Hunter  lecture delivers exclusive, cutting-edge insights that help you move beyond outdated assumptions and equip your team to interpret data with clarity and confidence.   In this session, you’ll gain:   ✅ A framework for understanding when apparent multiple affinities really matter—and when they don’t ✅ Guidance on extracting meaningful information from binding experiments that advance your work efficiently ✅ Clarity that helps you move from assay to decision faster, with fewer false starts   This isn’t textbook material—it’s real-world expertise designed to help you optimize faster and more effectively.     Move Faster, Smarter, and with Confidence   When you understand what your assays are truly showing you, you eliminate wasted effort and focus only on compounds with genuine potential.   Every day spent misunderstanding the meaning of apparent affinity differences can slow your project’s path to key milestones.   This is about accelerating your path from discovery to clinic, without wasted cycles or missteps.     Why the Myth of High and Low Affinity Binding Sites Could Be Slowing Your Pipeline   If you’re working in drug discovery, you know the pressure: timelines are tight, resources finite, and decisions must be fast and informed. Yet some assumptions still shaping pharmacology workflows haven’t evolved as fast as today’s science.   One of the most persistent misconceptions? The interpretation of high and low affinity binding sites  on GPCRs.   At first glance, when a ligand appears to bind at two different affinities in the same system, it seems logical to assume two distinct sites. But as Terry Kenakin reveals, this interpretation can be misleading, and sticking with it could slow your path to an optimized candidate.   High and Low Affinity: What’s Really Going On? It’s common to observe two apparent affinities for a ligand under certain experimental conditions. But are these differences really pointing to two physical sites?   Kenakin challenges this assumption and shows that what you’re seeing may reflect something entirely different.   In many systems, a ligand may appear to bind with very high affinity when it facilitates formation of ligand-receptor-G protein complexes —an observation that creates the illusion of multiple sites.   But this doesn’t necessarily reflect what’s happening in a physiological context, and misunderstanding this can introduce inefficiency into your decision-making process.   Are You Using Models That Slow You Down?   The analytical tools that shaped traditional affinity analysis were designed for simpler systems. Without appreciating their limitations, it’s easy to misinterpret affinity values, potentially leading to inefficient workflows.   Misunderstandings at this level can delay optimization cycles, result in wasted SAR iterations, or cause programs to focus on leads that won’t deliver—ultimately slowing your program’s forward momentum. Don’t let outdated interpretations slow your next program. Join Now — Access Immediate, Actionable Insight   You’ll gain the insight needed to:   Interpret complex binding data correctly Separate what matters from what misleads Make confident, efficient decisions that keep your pipeline moving forward, toward your next milestone. Unlock “Rethinking Affinity” Now Only in Terry's Corner _____ #GPCR #BindingAffinity #Pharmacology #DrugDiscovery #LeadOptimization #TerryKenakin #EmergingDrugHunter #EfficientDiscovery #PipelineAcceleration

Welcome GPCR Fans,   In GPCR-targeted drug discovery, precision isn’t optional—it’s a requirement. But precision isn’t just about clean data; it’s about interpreting what that data means. Subtle misinterpretation can quietly derail projects, slow timelines, and waste scarce resources. That’s why this week at Dr. GPCR , we’re focusing on the hidden risks that undermine progress and how the right frameworks can keep your pipeline moving forward. This is a preview of what Premium Members access every week: industry insights, event updates, jobs, and classified publications—curated for scientists who need fast, actionable intelligence. 🔍 This Week in Premium: Sneak Peek Dr. GPCR Premium Members this week gain curated, early access to: Industry insights : GPCRs and mRNA in drug discovery; new strategies for inflammatory disease treatment; growth strategies from Tectonic Therapeutics Upcoming events : Lab-in-the-Loop AI-powered hit discovery (July 29); 5th Transatlantic GPCR Symposium (Sept 3–4); neuroGPCR Symposium (Sept 17) Career opportunities : Lead/Senior Researcher at St. Jude; Postdoctoral Fellow at University of Copenhagen; PhD in proteomics and GPCR signaling in cancer at CRCM Must-read publications : AlphaFold3 benchmarking for GPCRs; new structural insights into peptide ligand activation All curated for speed, relevance, and immediate application—only for Premium Members. Terry’s Corner: Rethinking Affinity, A Critical Edge for Drug Hunters One of the most persistent misconceptions in pharmacology workflows? The interpretation of high and low affinity binding sites on GPCRs. At first glance, when a ligand binds at two different affinities in the same system, it seems logical to assume two distinct sites. But Terry Kenakin’s new Emerging Drug Hunter lecture reveals why this assumption can mislead even experienced teams . What’s Really Going On? Under certain experimental conditions, what appears to be a second high-affinity site may simply reflect kinetic factors—such as ligand-receptor-G protein complex formation—creating the illusion of multiple sites that aren’t physiologically relevant. This misunderstanding leads to: Inefficient structure-activity relationship (SAR) cycles Wasted optimization efforts Focus on leads that fail later in development In this exclusive session, Kenakin gives you the frameworks needed to interpret data correctly, eliminate wasted effort, and accelerate confident decisions. 🔒 Available only in Terry’s Corner - Premium Members get an exclusive discount Secure Your Access To Terry's Corner ➤ Why the Myth of Multiple Affinity Sites Slows You Down Traditional models that shaped affinity analysis were designed for simpler systems. If you’re not accounting for their limitations today, your team risks costly misinterpretations that delay optimization cycles and waste resources. Kenakin shows exactly how to separate what matters from what misleads—practical, real-world expertise designed to help teams move faster, smarter, and with greater confidence. Every day spent misunderstanding apparent affinity differences delays key milestones. 🗣️ “Thank you for bringing this (Principles of Pharmacology I) course with Dr. Kenakin. I wish Dr. GPCR the best for the sake of promoting more educational opportunities that are sorely needed in the field” — Dr. GPCR University Learner Celtarys Research Recap: Medicinal Chemistry Highlights You May Have Missed The pace of innovation in medicinal chemistry is accelerating—and if you missed this year’s ACSMEDI-EFMC Medicinal Chemistry Frontiers 2025 , you’re already behind. At this international meeting, leaders shared next-gen strategies shaping modern drug discovery: Prof. Ingo Hartung : State-of-the-art design of small molecule drugs, including PROTACs Dr. Wendy Young : Career insights and lessons from a leader in drug development and a champion for women in science Dr. Katerina Leftheris : New technologies overcoming peptide limitations with insights from both pharma and startup environments Read Maria Majellaro's Full Recap ➤ Lab Leadership Without Ego: A Model for R&D Success Scientific rigor doesn’t thrive in cultures defined by micromanagement or burnout. At Alkermes, Sokhom Pin built an in vitro pharmacology group from scratch—not just a lab, but a culture that encouraged curiosity, empowered people, and supported balance while delivering results. His leadership principles: Hire for attitude and team fit—not just credentials Design workflows that enable curiosity-driven research Support work-life balance without compromising scientific excellence His approach didn’t just create a productive lab—it accelerated outcomes and laid the cultural foundation for the next generation of biotech innovation. Get The Full Story ➤ Why Dr. GPCR Premium Membership Gives You an Edge Dr. GPCR Premium is designed for scientists who need the right intelligence, fast—without noise, distractions, or delays. Every week, members get: A full edition of GPCR Weekly News : jobs, events, papers, industry updates Exclusive discounts on Terry’s Corner  digital pharmacology courses Priority access to insights from major conferences, emerging research, and expert commentary Whether you’re a pharmacologist, biotech scientist, or team leader, Dr. GPCR Premium gives you an edge in a fast-moving field. FAQ: What’s Included, Who It’s For, Why Now What’s included? The complete Weekly News digest, jobs, upcoming events, classified industry intelligence, Courses, & Conference Presentations. Who is it for? Scientists, drug discovery teams, and pharmacologists who need curated, career-relevant updates. Why now? The field is evolving rapidly. Those acting on the right insights now will define the next wave of discovery. Don’t Fall Behind—Access the Edge You Need 👉 Access all the news and upcoming events ➤ Already a Premium Member? Access this week’s full Premium Edition here ➤ Hashtags: #GPCR #DrGPCR #BindingAffinity #Pharmacology #DrugDiscovery #LeadOptimization #TerryKenakin #EmergingDrugHunter #EfficientDiscovery #PipelineAcceleration

C1-inhibitor (C1INH) is a protease inhibitor present in plasma but not in isolated platelet suspensions Methods Platelets were isolated from healthy donor whole blood and then labeled with anti-CD62P and PAC1

explain in detail steps shared between the two sample preparation strategies, including expression and isolation

insulin secretion and activates G protein-coupled receptors with a different mechanism from the cis isomer

explain in detail steps shared between the two sample preparation strategies, including expression and isolation

Current research has focused on isolating when and how neuropeptide transmission occurs, as well as the

This realization isn’t isolated.

explore the differential mRNA profiles in inflammatory and healthy pulp tissues from the patients. hDPSCs isolated

Migration assays were performed using PBMCs isolated from these individuals in response to the synthetic

Zagzoog A et al ., In vitro and in vivo pharmacological activity of minor cannabinoids isolated from

Splenic B cells were isolated via magnetic-activated cell sorting (MACS).

Although such pheromone/receptor systems are likely to function in both mate choice and prezygotic isolation

measuring the way these cells scatter light and emit fluorescence, they can be identified, quantified and isolated

It's the opposite of a reactive approach, where problems are solved in isolation.

Axelrod Symposium: Plant-derived molecules acting on GPCRs Molecular characterization of recombinant LSDV isolates

Reviews, GPCRs, and more Isolation and functional identification of secretin family G-protein coupled

This article is about one big idea: GPCRs don’t act in isolation—they respond to the system they’re in

make clear that public health strategies must address polysubstance exposure, not just fentanyl in isolation

phytochemical-based drug discovery approach for combating multi-drug resistant Staphylococcus aureus Isolation

Three takeaways from this week’s feature: Stop firefighting:  Learn why solving isolated problems burns

midgut contractions Ligand-based analysis of the antifungal potential of phytosterols and triterpenes isolated

the transducer component of signal transduction that requires GTP is G-protein and was the first to isolate Kent Kobilka and Robert Joseph Lefkowitz for their work on GPCR function.[62–66] Lefkowitz was able to isolate

receptor: novel biophysical fragment screening using polymer-encapsulated nanodiscs Google DeepMind And Isomorphic

Morgan Healthcare Conference Isomorphic Labs Announces Strategic Multi-Target Research Collaboration

Selection of the libraries typically leads to the isolation of several hundred candidate hits, enriched

Endogenous l- to d-amino acid residue isomerization modulates selectivity between distinct neuropeptide

Structural and Molecular Insights into GPCR Function Endogenous l- to d-amino acid residue isomerization