Design and synthesis of fluorescent probes for GPR54
| Autor: | Nobutaka Fujii, Ryosuke Misu, Hiroaki Ohno, Shinya Oishi, Akira Hirasawa, Nahoko Ieda, Kei-ichiro Maeda, Masato Kaneda, Hiroko Tsukamura, Yoshihisa Uenoyama |
|---|---|
| Rok vydání: | 2014 |
| Předmět: |
Male
Kisspeptin GPR54 Clinical Biochemistry Pharmaceutical Science Neuropeptide CHO Cells Biochemistry Cell Line Receptors G-Protein-Coupled Flow cytometry law.invention Rhodamine Fluorescent probe Structure-Activity Relationship chemistry.chemical_compound Cricetulus Kisspeptins Confocal microscopy law Drug Discovery medicine Animals Humans Receptor Molecular Biology Fluorescent Dyes Dose-Response Relationship Drug Molecular Structure medicine.diagnostic_test Organic Chemistry Fluorescence Molecular biology RFamide Rats Cell biology chemistry Drug Design Injections Intravenous Molecular Medicine hormones hormone substitutes and hormone antagonists Receptors Kisspeptin-1 |
| Zdroj: | Bioorganic & Medicinal Chemistry. 22:3325-3330 |
| ISSN: | 0968-0896 |
| DOI: | 10.1016/j.bmc.2014.04.052 |
| Popis: | Kisspeptins are neuropeptides that induce the secretion of gonadotropin-releasing hormone via the activation of the cognate receptor, G-protein coupled receptor 54 (GPR54). The kisspeptin-GPR54 axis is associated with the onset of puberty and the maintenance of the reproductive system. In this study, several fluorescent probes have been designed and synthesized for rat GPR54 through the modification of the N-terminus of rat kisspeptins to allow for the visualization of the expression and localization of kisspeptin receptor(s) in living cells and native tissues. The tetramethylrhodamine (TMR) and rhodamine green (RG)-labeled kisspeptins exhibited good binding and agonistic activities towards GPR54, and the results of the application studies demonstrated that these fluorescent probes could be used effectively for the detection of GPR54 receptors in flow cytometry and confocal microscopy experiments. |
| Databáze: | OpenAIRE |
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