Design and synthesis of fluorescent probes for GPR54 |
| |
| Institution: | 1. Graduate School of Pharmaceutical Sciences, Kyoto University, Sakyo-ku, Kyoto 606-8501, Japan;2. Graduate School of Bioagricultural Sciences, Nagoya University, Nagoya 464-8601, Japan;3. Graduate School of Agricultural and Life Sciences, The University of Tokyo, Tokyo 113-8657, Japan;1. Romanian Academy, Institute of Physical Chemistry “Ilie Murgulescu”, Splaiul Independentei 202, 060021 Bucharest, Romania;2. Polymer Department, National R&D Institute for Chemistry and Petrochemistry ICECHIM, Splaiul Independentei 202, 060021 Bucharest, Romania;3. University POLITEHNICA of Bucharest, Faculty of Applied Chemistry and Materials Sciences, Polizu 1, 78126 Bucharest, Romania;1. Department of Physics, The University of Texas at Dallas, 800 W. Campbell Rd., PHY 36, Richardson, TX 75080, United States;2. Departments of Pharmacology, Oncology and Radiation Oncology, Laboratory of Molecular Stress Responses and the Simmons Comprehensive Cancer Center, University of Texas Southwestern Medical Center, ND2.210K 601 Forest Park Drive, Dallas, TX 75390-8807, United States;1. Department of Neurology and Geriatrics, Gifu University Graduate School of Medicine, Gifu, Japan;2. Department of Internal Medicine, Mino City Hospital, Mino, Japan;3. Department of Radiology, Gifu University Graduate School of Medicine, Gifu, Japan;4. Department of Neurology, Kyoto Prefectural University of Medicine, Kyoto, Japan |
| |
| Abstract: | 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. |
| |
| Keywords: | Fluorescent probe GPR54 Kisspeptin RFamide |
| 本文献已被 ScienceDirect 等数据库收录！ |
|
