ArticleEJNMMI research2017
New approaches for the reliable in vitro assessment of binding affinity based on high-resolution real-time data acquisition of radioligand-receptor binding kinetics.
Article in EJNMMI research, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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Who cites it
13 citing papers in PubMed.
- Development of a GPCR-binding ligand screening method using real-time interaction analysis on live cells.Biochemistry and biophysics reports · 2026Article
- A Novel Method for Real-Time Quantification of Radioligand Binding to Living Tumor CellsCancer biotherapy & radiopharmaceuticals · 2024Article
- New Allosteric Modulators of AMPA Receptors: Synthesis and Study of Their Functional Activity by Radioligand-Receptor Binding Analysis.International journal of molecular sciences · 2023Article
- Experimental Nuclear Medicine Meets Tumor Biology.Pharmaceuticals (Basel, Switzerland) · 2022Review
- Ionic strength-sensitive and pH-insensitive interactions between C-reactive protein (CRP) and an anti-CRP antibody.Biophysics and physicobiology · 2022Article
- A novel assay based on pre-equilibrium titration curves for the determination of enzyme inhibitor binding kinetics.European biophysics journal : EBJ · 2021Article
- Development of a Human Estrogen Receptor Dimerization Assay for the Estrogenic Endocrine-Disrupting Chemicals Using Bioluminescence Resonance Energy Transfer.International journal of environmental research and public health · 2021Article
- A live cell NanoBRET binding assay allows the study of ligand-binding kinetics to the adenosine APurinergic signalling · 2019Article
- SNAPshots of the MCHR1: a Comparison Between the PET-Tracers [Molecular imaging and biology · 2019Article
- Article
- Detecting ligand interactions in real time on living bacterial cells.Applied microbiology and biotechnology · 2018Article
- [ACS medicinal chemistry letters · 2018Article
- Structure-Affinity Relationships and Structure-Kinetics Relationships of Pyrido[2,1-f]purine-2,4-dione Derivatives as Human Adenosine AJournal of medicinal chemistry · 2017Article
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7 authors.
Funding
Abstract
backgroundResolving the kinetic mechanisms of biomolecular interactions have become increasingly important in early-phase drug development. Since traditional in vitro methods belong to dose-dependent assessments, binding kinetics is usually overlooked. The present study aimed at the establishment of two novel experimental approaches for the assessment of binding affinity of both, radiolabelled and non-labelled compounds targeting the A
resultsTwo novel real-time cell-binding approaches were successfully developed and established. Both experimental procedures were found to visualize the kinetic binding characteristics with high spatial and temporal resolution, resulting in reliable affinity values, which are in good agreement with values previously reported with traditional methods. Taking into account the lipophilicity of the A
conclusionsBoth kinetic binding approaches comprise tracer administration and subsequent binding to living cells, expressing the dedicated target protein. Therefore, the experiments resemble better the true in vivo physiological conditions and provide important markers of cellular feedback and biological response.
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