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Yamada, Shoya Division of Pharmaceutical Sciences, Okayama University Graduate School of Medicine, Dentistry and Pharmaceutical Sciences
Kawasaki, Mayu
Fujihara, Michiko Division of Pharmaceutical Sciences, Okayama University Graduate School of Medicine, Dentistry and Pharmaceutical Sciences
Watanabe, Masaki Division of Pharmaceutical Sciences, Okayama University Graduate School of Medicine, Dentistry and Pharmaceutical Sciences
Takamura, Yuta Division of Pharmaceutical Sciences, Okayama University Graduate School of Medicine, Dentistry and Pharmaceutical Sciences
Takioku, Maho Division of Pharmaceutical Sciences, Okayama University Graduate School of Medicine, Dentistry and Pharmaceutical Sciences
Nishioka, Hiromi Division of Pharmaceutical Sciences, Okayama University Graduate School of Medicine, Dentistry and Pharmaceutical Sciences publons researchmap
Takeuchi, Yasuo Division of Pharmaceutical Sciences, Okayama University Graduate School of Medicine, Dentistry and Pharmaceutical Sciences Kaken ID
Makishima, Makoto Division of Biochemistry, Department of Biomedical Sciences, Nihon University School of Medicine
Motoyama, Tomoharu Graduate School of Integrated Pharmaceutical and Nutritional Sciences, University of Shizuoka
Ito, Sohei Graduate School of Integrated Pharmaceutical and Nutritional Sciences, University of Shizuoka
Tokiwa, Hiroaki Department of Chemistry and Research Center of Smart Molecules, Rikkyo University
Nakano, Shogo Graduate School of Integrated Pharmaceutical and Nutritional Sciences, University of Shizuoka
Kakuta, Hiroki Division of Pharmaceutical Sciences, Okayama University Graduate School of Medicine, Dentistry and Pharmaceutical Sciences ORCID Kaken ID publons researchmap
Abstract
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.
Note
This document is the Accepted Manuscript version of a Published Work that appeared in final form in Journal of Medicinal Chemistry, copyright © American Chemical Society after peer review and technical editing by the publisher. To access the final edited and published work see https://doi.org/10.1021/acs.jmedchem.9b00995.
Published Date
2019-09-04
Publication Title
Journal of Medicinal Chemistry
Volume
volume62
Issue
issue19
Publisher
American Chemical Society
Start Page
8809
End Page
8818
ISSN
00222623
NCID
AA00702411
Content Type
Journal Article
language
英語
OAI-PMH Set
岡山大学
Copyright Holders
© 2019 American Chemical Society
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DOI
Web of Science KeyUT
Related Url
isVersionOf https://doi.org/10.1021/acs.jmedchem.9b00995
Citation
J. Med. Chem. 2019, 62, 19, 8809-8818 Publication Date:September 4, 2019 https://doi.org/10.1021/acs.jmedchem.9b00995
Funder Name
Japan Society for the Promotion of Science
助成番号
12J06716
16K18688
17K06931
18K14391