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Title: Design and synthesis of fluorescent probes for GPR54.
Authors: Kaneda, Masato
Misu, Ryosuke
Ohno, Hiroaki  kyouindb  KAKEN_id  orcid (unconfirmed)
Hirasawa, Akira  kyouindb  KAKEN_id  orcid (unconfirmed)
Ieda, Nahoko
Uenoyama, Yoshihisa
Tsukamura, Hiroko
Maeda, Kei-ichiro
Oishi, Shinya  kyouindb  KAKEN_id  orcid (unconfirmed)
Fujii, Nobutaka
Author's alias: 大石, 真也
Keywords: Fluorescent probe
Issue Date: 1-Jul-2014
Publisher: Elsevier BV
Journal title: Bioorganic & medicinal chemistry
Volume: 22
Issue: 13
Start page: 3325
End page: 3330
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.
Rights: © 2014 Elsevier Ltd.
This is not the published version. Please cite only the published version.
DOI(Published Version): 10.1016/j.bmc.2014.04.052
PubMed ID: 24857775
Appears in Collections:Journal Articles

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