Journal of Medicinal Chemistry p. 8809 - 8818 (2019)
Update date:2022-08-02
Topics:
Yamada, Shoya
Kawasaki, Mayu
Fujihara, Michiko
Watanabe, Masaki
Takamura, Yuta
Takioku, Maho
Nishioka, Hiromi
Takeuchi, Yasuo
Makishima, Makoto
Motoyama, Tomoharu
Ito, Sohei
Tokiwa, Hiroaki
Nakano, Shogo
Kakuta, Hiroki
Ligands for retinoid X receptors (RXRs), "rexinoids", are attracting interest as candidates for therapy of type 2 diabetes and Alzheimer's and Parkinson's diseases. However, current screening methods for rexinoids are slow and require special apparatus or facilities. Here, we created 7-hydroxy-2-oxo-6-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydronaphthalen-2-yl)-2H-chromene-3-carboxylic acid (10, CU-6PMN) as a new fluorescent RXR agonist and developed a screening system of rexinoids using 10. Compound 10 was designed based on the fact that umbelliferone emits strong fluorescence in a hydrophilic environment, but the fluorescence intensity decreases in hydrophobic environments such as the interior of proteins. The developed assay using 10 enabled screening of rexinoids to be performed easily within a few hours by monitoring changes of fluorescence intensity with widely available fluorescence microplate readers, without the need for processes such as filtration.
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