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This collaboration aims to amplify the visibility and adoption of Celtarys’ cutting-edge fluorescent ligand technology and accelerate the development of GPCR-targeted therapeutics. Celtarys Research develops high-quality, fluorescently labeled ligands and innovative chemical biology About Celtarys Research Celtarys Research is a biotech company based in Spain that specializes in the development with excellent affinity and pharmacological profiles, designed to advance GPCR-targeted assay development

blood-brain-barrier (BBB) and the complexity of the central nervous system (CNS) pose a challenge for developing Both orphan and well-characterized GPCRs are untapped opportunities for drug development targeting CNS Some of the advantages of using fluorescent ligands for this are: Live-cell imaging:  receptor-ligand Faster assay development: also speeds GPCR target validation. concerns and regulatory hurdles: Non-radioactive alternative to screening In the context of CNS drug development

Fortunately, several techniques and methodologies have been developed to support this process. receptors can provide valuable insights for structure-activity relationship (SAR) studies, informing the development To overcome these challenges, future directions include developing high-throughput techniques, better For instance, Heydenreich et al. (2023) developed a data science framework that combined mutagenesis Flipping the GPCR switch: Structure-based development of selective cannabinoid receptor 2 inverse agonists

Cam Sinh Lu ,   Karen Gregory ,  Lauren May ,  Andrea Vernall , et al. for their fantastic paper on Development New ligands and new GPCR behaviors that produce unique drug profiles (i.e. intracellular ligands and November 21st : Unconventional GPCR Ligands as Drugs. Exclusive Deal for Scientists in Developing Nations If you reside and work in a developing country, complete Development of Putative Bivalent Dicovalent Ligands for the Adenosine A1 Receptor GPCRs in Cardiology

Can we leverage structural and computational insights not just to explain receptor–ligand interactions after the fact, but to forecast outcomes and design ligands with new properties? To tackle these, the lab employs molecular docking, molecular dynamics simulations, and ligand-based When existing compounds are exhausted, bespoke ligands are designed and synthesized in-house. Common questions in the group include: Can we forecast ligand efficacy or selectivity?

In the case of fluorescent ligands , where a fluorescent tag is attached to a pharmacophore , the receptor Ligand-directed labelling strategies  are a newly developed way to attach a fluorescent tag to a GPCR Studying ligand-induced clustering and evaluating protein-protein interactions becomes possible if using At Celtarys, our GPCR fluorescent ligands are designed with a variety of photophysical properties to A Robust and Efficient FRET-Based Assay for Cannabinoid Receptor Ligands Discovery.

tested its validity as a fluorescent probe for Tag-lite® assays, where we used a set of 7 cannabinoid ligands Because Tag-lite® is based on FRET, we have collaborated with BMG Labtech to develop an application note It has been proven that when different ligands bind to the receptors the effects are different depending In this case, Terbium is used as donor and CELT-335 fluorescent ligand is used as acceptor. If you are interested in our ligands or technology, feel free to contact me anytime. References 1.

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

Allosteric modulators offer a promising approach for developing drugs that enhance or inhibit receptor a significant opportunity for developing allosteric modulators.  Understanding the evolutionary conservation of these residues can lead to the development of drugs that provides a foundation for the development of more targeted and effective drug therapies. Molecular determinants of ligand efficacy and potency in GPCR signaling.

designing assay cascades, setting go/no-go points, and de-risking programs from hit validation through development GPCR partner Celtarys Research has validated a TR-FRET assay for cannabinoid receptor ligands using their across chemokines and their receptors drive selectivity and promiscuity, paving the way for rational ligand Distinct Ligand Activation in NMBR Simulations show how two ligands differently activate class A GPCR

In this session, you’ll gain: ✅ A deeper understanding of how every ligand alters receptor conformation—and Ligands don’t just “bind”—they change  the receptor. Ligands may take hours to equilibrate , even when they look potent on paper. What If the Same Site Behaves Differently Depending on the Ligand? In this lecture, Kenakin lays out why no ligand binds without altering receptor conformation , and how

Maria Majellaro Now, she leads a team of talented chemists at Celtarys, developing fluorescent ligands GPCR on the company page . _______________ Keyword Cloud:   GPCR scientist network , career development , fluorescent ligands , GPCR training program , Dr.

The AlphaFold-predicted models revealed distinct ligand-binding site shapes, enabling the prioritization highly dynamic proteins and continuously adopt different conformations based on their interactions with ligands However, AlphaFold3 faces challenges with synthetic ligands, which are central to pharmaceutical development It excels in modeling interactions with natural ligands but struggles to generalize this accuracy to Ligand discovery from a dopamine D3 receptor homology model and crystal structure.

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

For this reason, GPCRs have been a focus of drug development for decades due to their role in regulating but recent breakthroughs in understanding allosteric modulation have opened up new avenues for drug development fully or partially dampen the receptor's functional response to the ligand (Wold, Chen et al. 2019). mechanisms Allosteric sites can differentially modulate G-protein and β-arrestin coupling, enabling the development biased signaling induced by intracellular allosteric agonists and establish a strong foundation for developing

This week’s edition links ligand mechanism to the decisions that shape affinity, efficacy, selectivity Each week we highlight the decisions that move GPCR projects forward—from pharmacology essentials to ligand  Studies on active-state GPCR ensembles and their transducer coupling, biased angiotensin receptor ligands For GPCRs, fluorescent ligands have quietly become one of the most versatile technologies—supporting Speed:  faster GPCR target validation and assay development.

New ligands and new GPCR behaviors that produce unique drug profiles (i.e. intracellular ligands and November 21st : Unconventional GPCR Ligands as Drugs. Exclusive Deal for Scientists Residing and Working in Developing Nations If you live and work  in a developing Advisory Board Generate:Biomedicines Announces Multi-Target Collaboration with Novartis to Discover and Develop Antibody-based Agonist and a Class A GPCR Regulating Hunger and Satiety OMass Therapeutics Expands Development

Gábor Turu, and László Hunyady for their research on Functional consequences of spatial, temporal and ligand pharmacology (affinity, efficacy, co-operativity) Mechanisms of action for new GPCR ligands Essentials for predicting activity Unique drug profiles from new ligands and GPCR behaviors GPCR Event Highlight therapy to prevent heart failure progression GPCR Binders, Drugs, and more Advances in GPCR-targeted drug development Announces EUR 60M Series B Financing to Advance a Pipeline of Novel GPCR-Modulating Therapies into Clinical Development

Learn the fundamentals of ligand activity, mechanism of action, and GPCR discovery strategy—all at your Arrestin2 binds β₁AR without ligand-induced activation, reshaping our understanding of biased signaling A new cell-based tool detects receptor activity and reveals endogenous ligands.   Whether you're decoding a hidden receptor state or hunting for the next orphan GPCR ligand, we're here

Plus, Celtarys explores ligand selection for better assays, and co-founder Dr. Sign Up for The Kenakin Brief Fluorescent Ligands vs. Radioligands – Assay Smarter Celtarys explores how fluorescent ligands enable safer, high-throughput Upgrade Your Screening Strategy Leadership in Ligand Design  – The Celtarys Origin Story   In  this founder

membrane-driven modulation of mGluR2, and a big headline, Novo Nordisk’s $2.2B deal with Septerna to develop   — A tale of detergent tails: GPCR activation beyond ligands .   A new commentary highlights how detergents and cholesterol shape mGluR2 activation—no ligand required

Pharmacology isn’t only about ligands, receptors, and downstream G protein signaling—it’s also about It’s about revealing therapeutic liabilities before  they derail development. Why System Sensitivity Matters Consider the signaling cascade: ligand binds receptor, receptor couples The quantitative strength of this cascade depends not just on the ligand, but also on the abundance and between a high-affinity/low-efficacy agonist  versus a high-efficacy agonist  before entering costly development

signaling architecture, and physiological feedback loops continuously rewrite the connection between ligand Allosteric Modulators: System-Conscious Control Orthosteric ligands displace native signaling and impose Endogenous ligands remain part of the signaling equation, preserving physiological patterning. Efficacy is not a molecule-only attribute—it's a joint property of ligand and system. This is why experts never classify ligands from a single system: The same molecule can occupy different

direct cell migration during immune surveillance and inflammation, as well as to play vital roles in the development , maturation, and homing of lymphocytes and the development of organs. receptors (CKRs) that signal via Gαi and 4 official atypical chemokine receptors (ACKRs) which engage in ligand sites, while maintaining the responsiveness of canonical G protein-coupled CKRs that bind to the same ligand CKRs should be considered when evaluating the safety and therapeutic efficacy of blocking receptor-ligand

The integration of AI in GPCR drug discovery has the potential to accelerate the identification and development Structure: the development of algorithms such DeepMind’s Alphafold2 (Jumper et al., 2021) and RoseTTAFold Open-source data: accessibility of databases to a wider audience will encourage the development of new Efforts will likely be made to develop AI models that can provide transparent explanations for their Precision medicines for GPCRs: AI can facilitate the development of personalized treatments by analyzing

Biased agonism is a phenomenon where different ligands acting on the same receptor trigger distinct signaling Biased agonism at the GLP-1R has been extensively studied, revealing that different ligands can stabilize Compared to the endogenous ligand GLP-1, another endogenous ligand, oxyntomodulin, exhibits a bias towards concept of biased agonism has been effectively leveraged in drug discovery, as demonstrated by the development By selectively targeting specific signaling pathways, it is possible to develop drugs with improved efficacy

At first glance, when a ligand appears to bind at two different affinities in the same system, it seems It’s common to observe two apparent affinities for a ligand under certain experimental conditions. 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.  

If you’re not there, you’re missing out on the next wave of allosteric modulators, biased ligands, and Corner, Yamina's Corner, biotech, systems thinking, signal transduction, operational excellence, drug development

with chemist Johannes Broichhagen aka JB, the goal was bold and elegant: Create a photo-switchable ligand Hodson: physiology, disease context, and imaging logic JB: chemistry, ligand engineering, mechanistic Collaboration, Chemistry, and the Pivot That Changed the Project Goal:  Develop a photo-switchable GPCR ligand Result:  The switching didn’t work Observation:  Binding + localization were unexpectedly robust