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Eleonora Comeo synthesizes fluorescent ligands to watch adenosine receptor pharmacology happen in living Ligands and the Pharmacology of Adenosine Receptors Adenosine receptors are among the most studied GPCRs ligands to address that gap directly - tools designed to visualize adenosine receptor pharmacology at SCIENTIFIC THEMES OF THE CONVERSATION Fluorescent ligands as pharmacological tools - how synthetic chemistry Visibility changes what pharmacology can ask Fluorescent ligands do more than confirm receptor binding

We have a catalogue of over 30 fluorescent ligands for different families of GPCRs, including adenosine Celtarys Research develops high-quality, fluorescently labeled ligands and innovative chemical biology “We’re thrilled to partner with Celtarys and introduce their high-performance fluorescent ligands to High Content Screening Service Live‑cell HCS imaging in HEK‑293T–hCB2R with fluorescent ligand CELT-331 Product Catalog GPCR Ligands Our GPCR fluorescent ligands are the ideal solution for your High Throughput

His group focuses on the development of chemical tools — including fluorescent ligands and photopharmacological screening services that enable fluorescence-based methods across drug discovery. The company's portfolio is built around high-affinity, selective fluorescent ligands for GPCRs, supporting Broad GPCR fluorescent ligand portfolio across multiple receptor families Fluorescence Polarization, services using proprietary probes in living cells Custom chemical development for probe and ligand creation

Discover how Celtarys Research is transforming GPCR assay development with fluorescent ligands in this At Celtarys, the focus is on enabling fast, customizable development of fluorescent ligands and chemical ligand development. “You can have a great ligand—but if you can’t solubilize it, it’s useless.” — Maria Majellaro Celtarys Their approach is highly consultative—they don’t just sell ligands, they co-develop solutions.

protein-coupled receptor kinetics, signaling, and trafficking and on using novel imaging techniques, such as fluorescent ligands and complementation methods, to investigate the underlying mechanisms.

His team develops fluorescence-based and chemically engineered tools to study gpcr internalization and ligand engagement in intact islets and neuronal circuits — insights that inform next-generation functional signaling in metabolic tissues What collaborative chemistry enabled in designing receptor-targeted fluorescent ligands The moment when structural and imaging evidence clarified unexpected glucagon-derived peptide

Chemical biologist Johannes Broichhagen reveals how fluorescent probes transform GPCR imaging, internalization Johannes Broichhagen shares how his lab builds next-generation fluorescent probes to visualize GPCRs chemical design can solve that antibodies can’t, how to validate functional assay systems, and why fluorescence-based Why peptide-based fluorescent ligands succeeded where antibodies repeatedly failed. at the Leibniz Research Institute for Molecular Pharmacology (FMP) in Berlin, focusing on developing fluorescent

How academia and biotech collaborate to scale GPCR tools—covering fluorescence assays, GPCR internalization The episode explores gpcr internalization , fluorescence-based probe design, and how functional assay Celtarys Research , a biotech spin-off from the University of Santiago de Compostela focused on advanced fluorescent ligands and GPCR research tools. By combining fluorophore design, ligand chemistry, and pharmacology, his work enables precise visualization

Discover pHSense™ portfolio From binding to signaling to internalization: Cell-based fluorescence assays for complete GPCR characterization The principle of pHSense™ relies on the pH-dependent fluorescence Time-Resolved Fluorescence (TRF) = High Signal-to-Background: Europium’s long-lived fluorescence allows comprehensive reagent portfolio to match that complexity—supporting every stage of the signaling pathway, from ligand Ligand binding Measure receptor engagement with high sensitivity using TR-FRET, radioligand, and Fluorescent

early discoveries in cyclic AMP signaling to uncovering ultrasensitive receptor responses at femtomolar ligand This conversation is especially valuable for scientists developing functional assays, fluorescence-based The moment when femtomolar ligand concentrations uncovered unexpected receptor sensitivity. Why It Might Hit Home If you’ve ever: Faced unexpected assay behavior at ultra-low ligand concentrations

three different functional units depending on which RAMP is present, and those distinctions determine ligand Each of the three RAMPs can pair with a given receptor to produce a distinct complex - different ligand RAMPs Act Allosterically - Not Through Direct Ligand Contact Structural data from the CLR and CTR receptor , and bimolecular fluorescence complementation in vivo 26:42 Structural data and what it reveals about Because we don't have selective ligands."

Understanding how ligand binding leads to specific signaling outcomes—particularly ligand bias toward can reproduce experimentally measured ligand bias. Episode Timeline 00:00 — Introduction: From ligand binding to receptor signaling Overview of ligand bias In GPCRs, a ligand binds at the extracellular side of the receptor. Ligands may bind one subtype strongly but another weakly.

With a career spanning two decades at the intersection of fluorescence chemistry, functional assays, Originally trained as a physicist with a strong interest in photophysics and fluorescence chemistry,

Listeners interested in GPCR drug discovery, functional assay development, or fluorescence-based assays If you want to expand high-throughput or fluorescence-based assay strategies to non-traditional models

We have developed an array of fluorescent biosensors to map kinase activity in living cells and are exploring

He currently uses high-resolution fluorescence microscopy and biochemistry to study GPCR trafficking

His current interests include the development of HTS fluorescence-based kinetic binding assays specifically

Cheloha builds nanobody-GPCR ligand conjugates that rescue weak peptides, engineer receptor selectivity Why do some ligands continue activating from the endosome while others don't? And can selectivity for one receptor subtype be engineered without redesigning the ligand from scratch His work has demonstrated that nanobody-ligand conjugates can rescue pharmacologically weak peptides, engineer receptor subtype selectivity, and open mechanistic questions that conventional ligand design

, cannabinoid receptor) and ion channel (K, Ca, TRP channel) function; mostly electrophysiology and fluorescence-based

Hill | Terry's Pharmacology Corner Topics Covered The biological basis of receptor signaling bias and ligand-dependent Why potency alone is not enough for candidate-level decisions 📅 May 28, 2026 at 3:00:00 PM Details Fluorescent

“Let’s embrace the challenge to study all of them… they’re unique in how they bind ligands, how selective With hundreds of subtypes and very few known ligands, the structure–function relationships remain largely “The main challenge was: how do we get a face for these proteins when we don’t have ligands?” Build predictive models to discover new ligands . Despite their relevance, they remain understudied due to the limited knowledge of their ligands and the

Drug Candidates G protein-coupled receptors can signal through multiple intracellular pathways, and ligands It is a consequence of ligand-dependent receptor conformations and allosteric probe dependence, and it The Biology Behind Bias Ligands produce differential pathway engagement at a single receptor because Multiple mechanisms of action: cAMP accumulation, β-arrestin recruitment, receptor internalization, ligand detection kits, and custom products Applications across target identification, HTS, lead optimization, ligand

Graciela Piñeyro on what happened when her lab tested biased agonism at the μ-opioid receptor across 25 ligands If the right ligand could engage G-protein signaling while sparing β-arrestin, pain relief might finally Across 25 ligands profiled at the μ-opioid receptor, the team found no bias, only partial agonism. from Pfizer — they could not identify a ligand-bias signature. The mechanistic story that guided a decade of biased-ligand drug discovery needs rebuilding from the

In addition, I generated various optical biosensors based on fluorescence or bioluminescence resonance

Maria Waldhoer on why endpoint GPCR assays miss most of what ligands do — and what kinetic pharmacological of InterAx Biotech AG, argues that endpoint assays — the field's default way of characterizing GPCR ligands , and into biotech at InterAx — where the next challenge is using functional fingerprints to design ligands Scientific Themes of the Conversation Kinetic versus endpoint characterization of GPCR ligands Systems of receptor signaling pathways Pharmacological fingerprints as multi-parameter compound descriptors Ligand

Our mission is to understand the mechanism and structural bases for ligand binding and efficacy to help This is an important perspective in the pursuit of receptor subtype-specific ligands, a major aspect One example of our recent work surrounds a structure-based effort to develop ligands that specifically Our goal is to develop safer beta2AR-selective ligands for the treatment of asthma and acute rescue therapy We have identified several GPCR ligands that allosterically modulate orthosteric ligand binding and target

Together with Irina Kufareva , UCSD, her team developed a novel approach to identifying ligands for orphan GPCRs by developing a powerful new computational tool for identifying ‘surrogate’ ligands (borrowed inaccessible receptors to well-characterized and understood ‘unlocked’ therapeutic targets with high-affinity ligands

family of membrane receptors, yet a significant portion remain orphans - proteins whose endogenous ligands to move from a bare protein sequence to a pharmacologically characterized receptor with identified ligands to the de-orphanization of GPR139 and GPR55, including the identification of sub-nanomolar peptide ligand He is one of the coordinators of recommendations to describe ligand bias towards signaling probes and His group recently developed an online resource of biased ligands and pathway effects to advance the

Lefkowitz , where his research focused on biased agonism, with the development of approaches to quantify ligand The chemokine system is relatively unique in having multiple receptors and multiple ligands that display His group and others have shown that many of these ligands act as biased agonists for the same receptor

They carry the characteristic seven-transmembrane topology, but their ligands are large, lipid-modified specificity across the 10 frizzled subtypes — each receptor is its own pharmacological entity The Wnt ligand problem — lipid modifications, carrier proteins, and what makes these ligands so difficult to work with The Wnt ligand problem may be the field's deepest bottleneck Wnt ligands are approximately 35–40 kDa, Fewer than one in 19 Wnt ligands is currently available in a biologically active, tagged form suitable