ArticleBritish journal of pharmacology2012
A novel fluorescent histamine H(1) receptor antagonist demonstrates the advantage of using fluorescence correlation spectroscopy to study the binding of lipophilic ligands.
Article in British journal of pharmacology, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 27 papers.
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Who cites it
27 citing papers in PubMed, 51 citations in OpenAlex.
- Measuring Membrane Protein Dynamics in Plant Roots Using Fluorescence Correlation Spectroscopy.Methods in molecular biology (Clifton, N.J.) · 2027Article
- A label-free cell-based screening identifies enhydrin as a novel natural antagonist of the histamine H1 receptor.Molecular diversity · 2026Article
- Design, Synthesis, and Characterization of Novel, Subtype-Selective Fluorescent Antagonists Targeting the Nociceptin/Orphanin FQ Opioid Peptide Receptor.Journal of medicinal chemistry · 2026Article
- Optimization of Peptide Linker-Based Fluorescent Ligands for the Histamine HJournal of medicinal chemistry · 2022Article
- Combined Free-Energy Calculation and Machine Learning Methods for Understanding Ligand Unbinding Kinetics.Journal of chemical theory and computation · 2022Article
- Chemical Probes for Histamine Receptor Subtypes.Current topics in behavioral neurosciences · 2022Article
- New Chemical Biology Tools for the Histamine Receptor Family.Current topics in behavioral neurosciences · 2022Article
- Detection of genome-edited and endogenously expressed G protein-coupled receptors.The FEBS journal · 2021Review
- Ligand-directed covalent labelling of a GPCR with a fluorescent tag in live cells.Communications biology · 2020Article
- Fluorescent HACS medicinal chemistry letters · 2020Article
- CRISPR-Mediated Protein Tagging with Nanoluciferase to Investigate Native Chemokine Receptor Function and Conformational Changes.Cell chemical biology · 2020Article
- Fluorescent ligands: Bringing light to emerging GPCR paradigms.British journal of pharmacology · 2020Review
- Development of novel fluorescent histamine HScientific reports · 2018Article
- High-Affinity Functional Fluorescent Ligands for Human β-Adrenoceptors.Scientific reports · 2017Article
- Protein-ligand (un)binding kinetics as a new paradigm for drug discovery at the crossroad between experiments and modelling.MedChemComm · 2017Review
- Pharmacological Characterization of Human Histamine Receptors and Histamine Receptor Mutants in the Sf9 Cell Expression System.Handbook of experimental pharmacology · 2017Review
- Use of a new proximity assay (NanoBRET) to investigate the ligand-binding characteristics of three fluorescent ligands to the humanPharmacology research & perspectives · 2016Article
- The use of fluorescence correlation spectroscopy to characterize the molecular mobility of fluorescently labelled G protein-coupled receptors.Biochemical Society transactions · 2016Review
- Detection of the secondary, low-affinity β1 -adrenoceptor site in living cells using the fluorescent CGP 12177 derivative BODIPY-TMR-CGP.British journal of pharmacology · 2014Article
- Review
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3 authors at 1 institution in 1 country.
Funding
Abstract
background and purposeFluorescent ligands facilitate the study of ligand-receptor interactions at the level of single cells and individual receptors. Here, we describe a novel fluorescent histamine H(1) receptor antagonist (mepyramine-BODIPY630-650) and use it to monitor the membrane diffusion of the histamine H(1) receptor. EXPERIMENTAL APPROACH: The human histamine H(1) receptor fused to yellow fluorescent protein (YFP) was transiently expressed in CHO-K1 cells. The time course of binding of mepyramine-BODIPY630-650 to the H(1) receptor was determined by confocal microscopy. Additionally, fluorescence correlation spectroscopy (FCS) was used to characterize the diffusion coefficient of the H(1) receptor in cell membranes both directly (YFP fluorescence) and in its antagonist-bound state (with mepyramine-BODIPY630-650). KEY
resultsMepyramine-BODIPY630-650 was a high-affinity antagonist at the histamine H(1) receptor. Specific membrane binding, in addition to significant intracellular uptake of the fluorescent ligand, was detected by confocal microscopy. However, FCS was able to quantify the receptor-specific binding in the membrane, as well as the diffusion coefficient of the antagonist-H(1) receptor-YFP complexes, which was significantly slower than when determined directly using YFP. FCS also detected specific binding of mepyramine-BODIPY630-650 to the endogenous H(1) receptor in HeLa cells. CONCLUSIONS AND IMPLICATIONS: Mepyramine-BODIPY630-650 is a useful tool for localizing the H(1) receptor using confocal microscopy. However, its use in conjunction with FCS allows quantification of ligand binding at the membrane, as well as determining receptor diffusion in the absence of significant bleaching effects. Finally, these methods can be successfully extended to endogenously expressed untagged receptors in HeLa cells.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.