Ertl, Fabian J. and Kopanchuk, Sergei and Dijon, Nicola C. and Veiksina, Santa and Tahk, Maris-Johanna and Laasfeld, Tonis and Schettler, Franziska and Gattor, Albert O. and Huebner, Harald and Archipowa, Nataliya and Koeckenberger, Johannes and Heinrich, Markus R. and Gmeiner, Peter and Kutta, Roger J. and Holliday, Nicholas D. and Rinken, Ago and Keller, Max (2024) Dually Labeled Neurotensin NTS1R Ligands for Probing Radiochemical and Fluorescence-Based Binding Assays. JOURNAL OF MEDICINAL CHEMISTRY, 67 (18). pp. 16664-16691. ISSN 0022-2623, 1520-4804
Full text not available from this repository. (Request a copy)Abstract
The determination of ligand-receptor binding affinities plays a key role in the development process of pharmaceuticals. While the classical radiochemical binding assay uses radioligands, fluorescence-based binding assays require fluorescent probes. Usually, radio- and fluorescence-labeled ligands are dissimilar in terms of structure and bioactivity, and can be used in either radiochemical or fluorescence-based assays. Aiming for a close comparison of both assay types, we synthesized tritiated fluorescent neurotensin receptor ligands ([H-3]13, [H-3]18) and their nontritiated analogues (13, 18). The labeled probes were studied in radiochemical and fluorescence-based (high-content imaging, flow cytometry, fluorescence anisotropy) binding assays. Equilibrium saturation binding yielded well-comparable ligand-receptor affinities, indicating that all these setups can be used for the screening of new drugs. In contrast, discrepancies were found in the kinetic behavior of the probes, which can be attributed to technical differences of the methods and require further studies with respect to the elucidation of the underlying mechanisms.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | G-PROTEIN; NEUROPEPTIDE-Y; RECEPTOR ANTAGONIST; AGONIST-BINDING; HIGHLY POTENT; ANALOGS; ANISOTROPY; COMPLEXES; PEPTIDES; DESIGN; |
| Subjects: | 500 Science > 540 Chemistry & allied sciences 500 Science > 570 Life sciences 600 Technology > 615 Pharmacy |
| Divisions: | Biology, Preclinical Medicine > Institut für Biophysik und physikalische Biochemie Chemistry and Pharmacy > Institute of Pharmacy Chemistry and Pharmacy > Institut für Physikalische und Theoretische Chemie > Chair of Physical Chemistry I > Prof. Dr. Patrick Nürnberger |
| Depositing User: | Dr. Gernot Deinzer |
| Date Deposited: | 29 Jul 2025 11:53 |
| Last Modified: | 29 Jul 2025 11:53 |
| URI: | https://pred.uni-regensburg.de/id/eprint/64307 |
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