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pharmacologists misinterpret how an antagonist interacts with its receptor, the consequences ripple across assay development, SAR interpretation, and clinical translation.

ligand mechanism to the decisions that shape affinity, efficacy, selectivity, safety, and downstream assays That subtle distinction opened the door to a brand-new assay format. Instead of imaging-heavy workflows, pHSense offers a no-wash, plate-reader–ready, high-throughput assay Cleaner data:  higher signal-to-noise ratios sharpen CNS assays. Speed:  faster GPCR target validation and assay development.

Progressive Technologies and Approaches Revealing Novel GPCR Biology and Drug Development Potential. FREE Symposium - IPI Surfacing (June 15, 2023) Training School on “Cell-based assays to study Adhesion - Antibody Engineering Scientist—Immuno-Oncology Convergent Research - Senior Scientist, Cell-Based Assay Development Explore Dr.

GPR37L1 controls maturation and organization of cortical astrocytes during development. Progressive Technologies and Approaches Revealing Novel GPCR Biology and Drug Development Potential. FREE Symposium - IPI Surfacing (June 15, 2023) Training School on “Cell-based assays to study Adhesion IRN I-GPCRNet (October 25 - 27, 2023) GPCR Jobs Convergent Research - Senior Scientist, Cell-Based Assay Development Post Doctoral Fellow Research associate in protein production Vice President, Oncology Clinical

Methods & Updates in GPCR Research NanoBiT- and NanoBiT/BRET-based assays allow the analysis of binding Progressive Technologies and Approaches Revealing Novel GPCR Biology and Drug Development Potential. FREE Symposium - IPI Surfacing (June 15, 2023) Training School on “Cell-based assays to study Adhesion - Antibody Engineering Scientist—Immuno-Oncology Convergent Research - Senior Scientist, Cell-Based Assay Development Explore Dr.

presented at the 23rd BioEquity Conference British Patient Capital Invests £10m in next-generation drug development Progressive Technologies and Approaches Revealing Novel GPCR Biology and Drug Development Potential. FREE Symposium - IPI Surfacing (June 15, 2023) Training School on “Cell-based assays to study Adhesion - Antibody Engineering Scientist—Immuno-Oncology Convergent Research - Senior Scientist, Cell-Based Assay Development Explore Dr.

Progressive Technologies and Approaches Revealing Novel GPCR Biology and Drug Development Potential. FREE Symposium - IPI Surfacing (June 15, 2023) Training School on “Cell-based assays to study Adhesion Antibody Engineering NEW Scientist—Immuno-Oncology Convergent Research - Senior Scientist, Cell-Based Assay Development Post Doctoral Fellow Research associate in protein production Vice President, Oncology Clinical

October 2022 "We describe production of the human A2A adenosine receptor (A2AAR), a class A G protein-coupled receptor (GPCR) for 19F-NMR and single-molecule fluorescence (SMF) spectroscopy. We explain in detail steps shared between the two sample preparation strategies, including expression and isolation of A2AAR and assembly of A2AAR in lipid nanodiscs and procedures for incorporation of either 19F-NMR or fluorescence probes. Protocols for SMF experiments include sample setup, data acquisition, data processing, and error analysis. For complete details on the use and execution of this protocol, please refer to Wei et al. (2022) and Sušac et al. (2018)." Read more at the source #DrGPCR #GPCR #IndustryNews

Pipeline Efficiency Begins With the Chemistry Itself Drug discovery pipelines often stall not because the target is wrong—but because the chemical matter  interacting with that target lacks the right properties to produce meaningful pharmacology. We obsess over target validation, signaling pathways, expression patterns, and disease relevance. Yet, far less time is spent scrutinizing the structural logic and origin  of the molecules we screen in the first place. This lesson asks a deceptively simple question: What if our molecules—not our targets—are limiting discovery? In this lesson, you’ll gain: A strategic view of how chemical scaffolds shape pharmacologic outcomes An understanding of new chemical sources beyond natural agonist analogs Awareness of how GPCR allostery and biased signaling are redefining drug design The Long Arc of Chemical Pharmacology The early history of drug discovery was rooted in nature . Extracts from plants, fungi, bacteria, and environmental microorganisms provided the first potent modulators of physiology. Opium, for example, was used for dysentery and relief of suffering as early as the 3rd century BC; its derivatives — morphine, codeine, papaverine — became cornerstones of modern therapy.  The natural world still holds enormous untapped potential . Less than ~15% of higher plant species, <5% of bacterial and fungal species, and only a fraction of marine organisms have been meaningfully explored.  Yet natural-product scaffolds come with costs: they are structurally complex, expensive to modify, often unpredictable in IP , and sometimes more difficult to optimize for modern pharmacokinetics.  Still, nature remains a treasure map — just one that requires more strategic navigation. The key question Terry raises: If natural scaffolds provided our starting pharmacology, what new scaffolds will define the next 50 years? Building on Known Pharmacology Medicinal chemists learned early that modifying endogenous molecules — hormones, neurotransmitters, and metabolic signals — could yield new drug effects. Adenine-derived scaffolds enabled selective adenosine receptor antagonists; tryptophan modifications led to somatostatin receptor ligands.  From these efforts emerged the concept of privileged structures : chemical backbones that show repeat utility  across GPCR classes and receptor families. Indoles, benzodiazepines, phenethylamines — each recurs because it “fits” biology well.  This was more than trial-and-error. It was early structure-based pharmacology. Dr. Kenakin highlights how hybrid molecules  — combining two pharmacophores into one scaffold — enable dual-modality treatments with unified pharmacokinetics  (instead of juggling two separate drugs with mismatched ADME profiles).  And occasionally, new chemistry emerges from an unexpected source: Side effects. Diuretic action discovered in sulfanilamide derivatives led to furosemide; sedative effects of early antihistamines helped launch antipsychotics.  Lesson:  The structure-response relationship is rarely linear — and observing the unexpected is part of the craft. Informatics Expands the Search Space for Chemical Drug Matter Advances in chemoinformatics  introduced large-scale similarity mapping, such as SEA (Similarity Ensemble Approach), which compares the chemical similarity of ligands , not the protein sequence of targets.  This is a philosophical shift: Instead of asking, “Which proteins are related?” We ask, “Which molecules behave as if they belong together?” This approach reveals: Hidden target overlap New therapeutic hypotheses “Off-target” effects that may be on-target opportunities This expands drug matter beyond the familiar and encourages deliberate exploration of chemical novelty, rather than incremental tuning of existing scaffolds. The molecule, not the receptor, becomes the guiding principle. Allostery and Biased Signaling Change the Game The most profound change in GPCR drug discovery is our expanding understanding of allosteric receptor function . GPCRs are not simple on/off switches. They are allosteric machines , able to shift conformational states in response to multiple binding influences.  This enables: Positive Allosteric Modulators (PAMs) — enhance natural signaling Negative Allosteric Modulators (NAMs) — attenuate signaling Biased agonists  — favor one intracellular pathway over another These are not analogs of natural transmitters. They are structural strategies for tuning physiology. This reroutes discovery toward: Functionally selective ligands Better therapeutic windows More predictable clinical behavior Allosteric modulation allows us to work with  biology’s dynamic systems instead of forcing orthosteric competition. Biologics Are Now Chemical Drug Matter, Too Proteins, peptides, and antibodies are no longer niche. They are mainstream pharmacology. They offer high specificity , favorable safety , and unique mechanisms , including GPCR modulation through agonism, internalization, or ligand scavenging.  Advances in formulation and delivery have overcome earlier pharmacokinetic limitations. Peptide GPCR therapies now address obesity, diabetes, cancer, neuroendocrine disorders, inflammatory diseases, and more.  The boundary between “small molecule” and “biologic” has blurred. What matters now is not the category , but the fit: Does the chemical matter support the therapeutic mechanism? Does it interact with the receptor in a way that biology can use? Core message: The receptor is only half the story. The molecule is the other half. Why Terry’s Corner Terry’s Corner is a continuously growing knowledge platform built for scientists who want sharper decision-making power in discovery pharmacology. Subscribers gain weekly lectures led by Dr. Terry Kenakin, monthly AMA discussions, and on-demand access to a library of expert GPCR teaching sessions. Members can also propose new topics, ensuring relevance to real-world discovery problems. This is strategic, method-proven insight for discovery teams, pharmacologists refining core skills, and R&D leads who need clear reasoning in a rapidly changing field. GPCR innovation is accelerating. Those who learn now will shape the drugs others spend the next decade trying to understand. 40 years of expertise at your fingertips: Explore the full library ➤ Subscribe to the Kenakin Brief to stay in the know ➤

Recent studies have revealed that PGs play pivotal roles in embryo development, ciliogenesis, and organ During development, PGE2 signaling regulates embryogenesis, hepatocyte differentiation, hematopoiesis advances in understanding the functions and mechanisms of prostaglandin signaling in ciliogenesis, embryo development

Developmental and homeostatic signaling transmitted by the G-protein coupled receptor FPR2. Progressive Technologies and Approaches Revealing Novel GPCR Biology and Drug Development Potential. FREE Symposium - IPI Surfacing (June 15, 2023) Training School on “Cell-based assays to study Adhesion I-GPCRNet (October 25 - 27, 2023) GPCR Jobs NEW Convergent Research - Senior Scientist, Cell-Based Assay Development NEW Post Doctoral Fellow NEW Research associate in protein production NEW Vice President

December 2021 "Drug development is rarely trivial. typically require years to uncover the mechanisms of disease before they can even dare to contemplate the development Nevertheless, researchers have a host of new technologies at their disposal to develop targeted therapies Modern drug development approaches include a range of techniques leveraging structural biology, immunology

. ✅ Practical ways  to integrate kinetics, allostery, and bias into smarter development decisions. ✅ The real friction point lies downstream : translating receptor–ligand interactions into actionable development Early In Vivo Wins the Race When is the right time to move beyond cell assays? How CRO Communication Impacts GPCR Drug Development Success Even the best science falters without operational Direct input  on future sessions—so topics match the hurdles your team faces in discovery and development

You can have the most brilliant minds and cutting-edge assays, but if your science isn't continuously My work isn't just  about the latest and best assay; it's about the framework that ensures the right assay data leads to the right decision. We'll look at how overlooked operational details, such as misaligned data from diverse GPCR assay types

A number of strategies have been applied to develop CB2 ligands to achieve closer to 'drug-like' properties We review the current state of CB2 ligand development and progress in optimising physicochemical properties

A number of strategies have been applied to develop CB2 ligands to achieve closer to 'drug-like' properties We review the current state of CB2 ligand development and progress in optimizing physicochemical properties

pHSense™ reagents enable real-time GPCR internalization detection A breakthrough GPCR internalization assay Developed to address long-standing challenges in GPCR internalization assays , pHSense™ reagents  combine Eric Trinquet, Director of Research and Development at Revvity.   innovation , pHSense™  was developed to overcome three persistent barriers in internalization studies  and the scientific “aha” moments that drove its development.

to identify compounds that interact with molecular targets involved in disease pathways is where the development Target-based screening is now a fundamental pillar of drug development, and GPCRs are key targets for How Fluorescence Polarization Assays Work: Principles and Applications in GPCR Research FP assays work FP assays are convenient and easy to manipulate. polarization technology is expected to expand its role in GPCR research through the development of novel

Today, InterAx Biotech is pleased to announce that Carola Weiss has joined the company as VP Business Development Carola Weiss’ professional career brings deep expertise in business development, marketing & sales, licensing

(Nasdaq: TRVN), a biopharmaceutical company focused on the development and commercialization of novel patients with central nervous system (CNS) disorders, today announced it is advancing TRV045 into clinical development TRV045 is the Company’s novel S1P1 receptor modulator being developed as a potential treatment for diabetic

fibrosis, cancers, cardiovascular diseases and neuropathic pain, making it a promising target for drug development This article provides an extensive review on the current status of ligand development targeting LPA receptors

a set of 7 cannabinoid ligands (both natural and synthetic) to validate and optimize the assay. Because Tag-lite® is based on FRET, we have collaborated with BMG Labtech to develop an application note It bears a hydrophilic fluorophore compatible with the terbium donor in TR-FRET assays. Figure 2.Assay Principle: TR-FRET assay using CELT-335, a dual (CB1/CB2) fluorescent ligand that serves Comparison of binding affi nities using radioligand binding or TR-FRET assays.

January 2022 Exscientia and Sanofi Establish Strategic Research Collaboration to Develop AI-driven Pipeline Sanofi and Exscientia announced today a groundbreaking research collaboration and license agreement to develop

It was simply a clean, scalable assay—and a wave of new possibilities. That’s the promise of pHSense, a groundbreaking reagent developed by Eric Trinquet and his team at Revvity This was the foundation of a new set of assay tools. Mini Timeline: pHSense Development Early 2020s: Rare-earth probe synthesis begins Collaborative screening User feedback will guide the development of future tags and variants.

Maria Majellaro, highlighting their fluorescent ligand tools for live-cell GPCR assays.   Maria Majellaro of Celtarys shares how her team translates medicinal chemistry into practical GPCR assay Introducing Celtarys - Probe Development via Conjugation Strategies   Celtarys Research's first article provides a detailed examination of conjugation strategies to develop high-performance fluorescent probes It emphasizes scaffold selection, linker optimization, and assay compatibility to enhance target binding

December 2022 Sosei Heptares Enters Antibody Discovery Agreement with Twist Bioscience to Discover and Develop (“the Company”; TSE: 4565), the world leader in GPCR-focused structure-based drug design (SBDD) and development

June 2022 "We’re delighted to welcome Dr Ed Brennan as our new Vice President, Head of Clinical Development Dr Brennan has extensive experience across all phases of clinical development, and across multiple therapeutic

medicinal chemistry paved the way to co-founding Celtarys , a company now shaping the future of GPCR assay Over time, she developed a fascination with how molecules influence biology and how that chemistry could The academic group Maria worked with had developed a technology that allowed for flexible, fast synthesis GPCR, is helping researchers worldwide gain access to customized, reliable assay tools without the delays and frustrations that often plague probe development. 👉 Learn more about Celtarys’ science-driven solutions

November 2021 Twist Bioscience Launches Revelar Biotherapeutics to Develop and Commercialize Novel COVID Executive Leadership Team Established with Demonstrated Success in Clinical, Regulatory and Commercial Development has launched Revelar Biotherapeutics, Inc., an independently operated, new biotechnology company to develop

Yamina’s Corner opens for strategic consulting, and our partner Celtarys unveils a robust TR-FRET assay Yamina’s Corner delivers GPCR consulting that cuts through the noise, designing assay cascades, setting go/no-go points, and de-risking programs from hit validation through development candidate selection Visit Yamina’s Corner Now CELT-335 - Celtarys Validates New Assay for CB1/CB2 Screening Dr. GPCR partner Celtarys Research has validated a TR-FRET assay for cannabinoid receptor ligands using their