2014年7月
Design and synthesis of fluorescent probes for GPR54
BIOORGANIC & MEDICINAL CHEMISTRY
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- 巻
- 22
- 号
- 13
- 開始ページ
- 3325
- 終了ページ
- 3330
- 記述言語
- 英語
- 掲載種別
- 研究論文(学術雑誌)
- DOI
- 10.1016/j.bmc.2014.04.052
- 出版者・発行元
- PERGAMON-ELSEVIER SCIENCE LTD
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. (C) 2014 Elsevier Ltd. All rights reserved.
- リンク情報
- ID情報
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- DOI : 10.1016/j.bmc.2014.04.052
- ISSN : 0968-0896
- eISSN : 1464-3391
- PubMed ID : 24857775
- Web of Science ID : WOS:000337215900012