期刊
ACS MEDICINAL CHEMISTRY LETTERS
卷 11, 期 1, 页码 16-22出版社
AMER CHEMICAL SOC
DOI: 10.1021/acsmedchemlett.9b00462
关键词
Neurotensin receptor; carbamoylated arginine; fluorescence labeling; flow cytometry; high-content imaging; confocal microscopy
资金
- Deutsche Forschungsgemeinschaft (DFG) [KE 1857/1-1, KE 1857/1-2]
- DFG [GRK 1910]
- International Doctoral Program Receptor Dynamics Elite Network of Bavaria
- BBSRC [1644276] Funding Source: UKRI
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.
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