Kaneda Masato, Misu Ryosuke, Ohno Hiroaki, Hirasawa Akira, Ieda Nahoko, Uenoyama Yoshihisa, Tsukamura Hiroko, Maeda Kei-ichiro, Oishi Shinya, Fujii Nobutaka
Graduate School of Pharmaceutical Sciences, Kyoto University, Sakyo-ku, Kyoto 606-8501, Japan.
Graduate School of Bioagricultural Sciences, Nagoya University, Nagoya 464-8601, Japan.
Bioorg Med Chem. 2014 Jul 1;22(13):3325-30. doi: 10.1016/j.bmc.2014.04.052. Epub 2014 May 5.
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.
亲吻素是一类神经肽，可通过激活同源受体——G蛋白偶联受体54（GPR54）来诱导促性腺激素释放激素的分泌。亲吻素-GPR54轴与青春期的启动及生殖系统的维持相关。在本研究中，通过对大鼠亲吻素的N端进行修饰，设计并合成了几种用于大鼠GPR54的荧光探针，以便在活细胞和天然组织中可视化亲吻素受体的表达和定位。四甲基罗丹明（TMR）和罗丹明绿（RG）标记的亲吻素对GPR54表现出良好的结合和激动活性，应用研究结果表明，这些荧光探针可有效地用于流式细胞术和共聚焦显微镜实验中GPR54受体的检测。
