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.
View MoreWinchem Industrial Co. Ltd.(expird)
Contact:86-574-83851061 86-574-87083208
Address:Room 905, No.3 Building,East Business Center, 456 Xingning Road, Ningbo City,China
ShangHai Ruiyi Medical Technology Co.,Ltd.
Contact:+86-21-54718086
Address:No951 Jianchuan RD,Minhang District
Shuanghe Bio-Technology Limited(expird)
Contact:+86-571-61710758,18968016640
Address:Jinqiao north road 916# Fuyang
Jintan City Mego Chemical Co., Ltd
Contact:+86-0519-82814387
Address:23# Dengguan Town, Jintan, Jiangsu Province, China
Tangshan Moneide Trading Co., Ltd.
Contact:+86-315-8309571
Address:2-7-420 Jidong Building Materials Commercial Center, Tangshan, Hebei, 064000 China
Doi:10.1016/j.molliq.2020.114370
(2020)Doi:10.1248/cpb.33.2403
(1985)Doi:10.1055/s-1995-3940
(1995)Doi:10.1021/ja00397a040
(1981)Doi:10.1021/jo01093a005
(1959)Doi:10.1007/BF00760683
()