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Ligand-dependent intracellular trafficking of the G protein-coupled P2Y6 receptor. NMR applications to GPCR recognition by peptide ligands. Application of computational methods for class A GPCR Ligand discovery. New paradigms in purinergic receptor ligand discovery. Computational insights into ligand-induced G protein and β-arrestin signaling of the dopamine D1 receptor

These include infrared fluorescence, electrochemiluminescence, fluorescence emission, immunofluorescence staining, HTRF (homogeneous time-resolved fluorescence), and TR-FRET (time-resolved fluorescence resonance

When AUR is oxidized by APEX2 in the presence of H 2 O 2 , it produces a fluorescent product that can This fluorescence serves as a readout for the activity of APEX2 and, by extension, the trafficking of

Watch Episode 171 What happens when your protein has no known ligands, no structure, and very little The Problem: Hundreds of Receptors, Almost No Ligands Alessandro’s work focuses on olfactory GPCRs—nearly Most have only one known ligand, if any. That meant simulations, ligand screening, and experimental design could move forward with confidence. More accurate hypotheses, faster ligand discovery, and new strategies to tackle one of biology’s most

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?

Tracer concentration, receptor density, equilibrium assumptions, and ligand kinetics all influence whether Maria Majellaro, Johannes Broichhagen, and David Hodson discuss GLP-1 receptor probes, fluorescence-based

Optogenetic Microwell Array Screening System: A High-Throughput Engineering Platform for Genetically Encoded Fluorescent and Exhibition March 5 - 7, 2024 | 3rd GPCRs - Targeted Drug Discovery Summit March 23 - 24, 2024 | Ligand Recognition and Molecular Gating Seminar March 24 - 29, 2024 | Ligand Recognition and Molecular Gating

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

analyzed the lateral dynamics of the serotonin1A receptor in cholesterol-depleted cells (using statins) by fluorescence recovery after photobleaching (FRAP) and fluorescence loss in photobleaching (FLIP) measurements.

application Imaging GPCR Dimerization in Living Cells with Cucurbit[7]uril and Hemicyanine as a "Turn-On" Fluorescence in Pharmacology and Drug Discovery March 13 - 15 | 9th German Pharm-Tox Summit March 23 - 24, 2024 | Ligand Recognition and Molecular Gating Seminar March 24 - 29, 2024 | Ligand Recognition and Molecular Gating

vivo via differential phosphorylation Increased transcriptional elongation and RNA stability of GPCR ligand systematic approach of chemical intervention Methods & Updates in GPCR Research ORP9-PH domain-based fluorescent

energy landscape between thermodynamically coupled networks of amino acids from perturbations such as ligand Ligands binding to GPCRs can stabilise a distinct set of conformations, which promotes a certain pattern results of previous studies determining the 5-HT2AR structure, its molecular interactions with various ligands R luc: Renilla  luciferase, GFP: Green Fluorescent Protein. Fluorescent Tags Are Basically Never Silent. In the Pipeline  (Science, 2024).  

Lyu, Brian Shoichet, Bryan Roth, et al. for their research on AlphaFold2 structures guide prospective ligand regulates the self-renewal and pluripotency of mouse embryonic stem cells via JAK1/STAT3 signal pathway A fluorescently-tagged of the Prototypic G Protein-Coupled Adenosine A2A Receptor AlphaFold2 structures guide prospective ligand

al. for their research on Virtual Screening of a Chemically Diverse "Superscaffold" Library Enables Ligand Binders, Drugs, and more Virtual Screening of a Chemically Diverse "Superscaffold" Library Enables Ligand vertebrates Methods & Updates in GPCR Research Exploring GPCR conformational dynamics using single-molecule fluorescence

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

novel ligands for the A 2A  adenosine receptor. function and ligand-receptor interactions. Structure-based discovery of A2A adenosine receptor ligands. The directed evolution of ligand specificity in a GPCR and the unequal contributions of efficacy and Molecular determinants of ligand efficacy and potency in GPCR signaling.

Trinquet joined Cisbio in the early 2000s, working on what would become HTRF—Homogeneous Time-Resolved Fluorescence It reflects decades of foundational R&D—from the fluorescent probes of Cisbio’s early days to the receptor-targeting

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

,  Andrea Vernall , et al. for their fantastic paper on Development of Putative Bivalent Dicovalent Ligands New ligands and new GPCR behaviors that produce unique drug profiles (i.e. intracellular ligands and November 14th : The Application of GPCR Ligand Kinetics to Candidate Design. November 21st : Unconventional GPCR Ligands as Drugs. December 5th : Unique Exploitable GPCR-Ligand Behaviors for Therapeutic Benefit.

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

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.  

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.

This lesson helps you reframe how you interpret allosteric interactions —not as simple ligand displacement If your project involves GPCRs , functional selectivity , or non-traditional ligands , this session is In This Session, You’ll Gain: ✅ A clear explanation of why allosteric modulators don’t displace ligands—they allosteric cube The Allosteric Shift: When Receptors Become Something New In orthosteric pharmacology, a ligand No matter how much non-radioactive ligand you add, the binding curve levels off —because the receptor

thoroughly investigated the role of single amino acid changes to clarify the molecular mechanisms governing ligand Alternatively, allosteric modulators , which bind to sites outside the traditional ligand-binding pocket Interestingly, only 10 out of 82 important residues are within the ligand-binding pocket, resulting in By pinpointing the molecular determinants of ligand efficacy and potency in GPCR signalling, this research Molecular determinants of ligand efficacy and potency in GPCR signaling.

microbial metabolites and GPCRome in Alzheimer's disease Methods & Updates in GPCR Research Single-chain fluorescent mapping G-protein-coupled receptor agonists Development of a synthetic relaxin-3/INSL5 chimeric peptide ligand

The G protein and intracellular Ca2+ were detected, respectively, by qPCR and Fluo-4AM Ca2+ fluorescent

private group Certificate of participation Learn the essentials: Measuring the pharmacologic activity of ligands (affinity, efficacy, co-operativity) Determining mechanisms of action for new GPCR ligands Elements and effective GPCR discovery Master advanced applications: Using new cellular assays to analyze GPCR ligand behavior Predicting activity and in vivo target coverage with real-time kinetics Discovering new ligands

Unlike orthosteric ligands that bind directly to the receptor's active site, allosteric modulators target functional and/or affinity for an orthosteric ligand; and negative allosteric modulators (NAMs), that fully or partially dampen the receptor's functional response to the ligand (Wold, Chen et al. 2019). Alternatively, they can function as neutral allosteric ligands (NALs), binding to a receptor's allosteric site without causing any detectable alterations in the receptor or orthosteric ligand behavior (Lindsley

Registrants will learn: The powerful applications of new cellular assays to determine GPCR ligand behavior New ligands and new GPCR behaviors that produce unique drug profiles (i.e. intracellular ligands and November 14th : The Application of GPCR Ligand Kinetics to Candidate Design. November 21st : Unconventional GPCR Ligands as Drugs. December 5th : Unique Exploitable GPCR-Ligand Behaviors for Therapeutic Benefit.

September 5th to 26th, 2024 Registrants will learn: Essentials of measuring pharmacologic activity of ligands Application of this knowledge to determine the mechanism of action of new GPCR ligands. 31st, 2024 Registrants will learn: The powerful applications of new cellular assays to determine GPCR ligand New ligands and new GPCR behaviors that produce unique drug profiles (i.e., intracellular ligands and receptor subtypes Structural insights into ligand recognition, selectivity, and activation of bombesin