Keller, Max and Mahuroof, Shahani A. and Yee, Vivyanne Hong and Carpenter, Jessica and Schindler, Lisa and Littmann, Timo and Pegoli, Andrea and Huebner, Harald and Bernhardt, Guenther and Gmeiner, Peter and Holliday, Nicholas D. (2020) Fluorescence Labeling of Neurotensin(8-13) via Arginine Residues Gives Molecular Tools with High Receptor Affinity. ACS MEDICINAL CHEMISTRY LETTERS, 11 (1). pp. 16-22. ISSN 1948-5875,
Full text not available from this repository. (Request a copy)Abstract
Fluorescence-labeled receptor ligands have emerged as valuable molecular tools, being indispensable for studying receptor-ligand interactions by fluorescence-based techniques such as high-content imaging, fluorescence microscopy, and fluorescence polarization. Through application of a new labeling strategy for peptides, a series of fluorescent neurotensin(8-13) derivatives was synthesized by attaching red-emitting fluorophores (indolinium- and pyridinium-type cyanine dyes) to carbamoylated arginine residues in neurotensin(8-13) analogues, yielding fluorescent probes with high NTS1R affinity (pKi values: 8.15-9.12) and potency (pEC(50) values (Ca2+ mobilization): 8.23-9.43). Selected fluorescent ligands were investigated by flow cytometry and high-content imaging (saturation binding, kinetic studies, and competition binding) as well as by confocal microscopy using intact CHO-hNTS(1)R cells. The study demonstrates the applicability of the fluorescent probes as molecular tools to obtain, for example, information about the localization of receptors in cells and to determine binding affinities of nonlabeled ligands.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | PROTEIN-COUPLED RECEPTORS; LIGAND-BINDING; NEUROPEPTIDE-Y; GPCR LIGANDS; CANCER; INTERNALIZATION; PHARMACOLOGY; EXPRESSION; PEPTIDE; ASSAY; Neurotensin receptor; carbamoylated arginine; fluorescence labeling; flow cytometry; high-content imaging; confocal microscopy |
| Subjects: | 600 Technology > 615 Pharmacy |
| Divisions: | Chemistry and Pharmacy > Institute of Pharmacy |
| Depositing User: | Dr. Gernot Deinzer |
| Date Deposited: | 09 Apr 2021 07:16 |
| Last Modified: | 09 Apr 2021 07:16 |
| URI: | https://pred.uni-regensburg.de/id/eprint/45358 |
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