PMID- 31483660
OWN - NLM
STAT- MEDLINE
DCOM- 20200615
LR  - 20200615
IS  - 1520-4804 (Electronic)
IS  - 0022-2623 (Linking)
VI  - 62
IP  - 19
DP  - 2019 Oct 10
TI  - Competitive Binding Assay with an Umbelliferone-Based Fluorescent Rexinoid for 
      Retinoid X Receptor Ligand Screening.
PG  - 8809-8818
LID - 10.1021/acs.jmedchem.9b00995 [doi]
AB  - 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.
FAU - Yamada, Shoya
AU  - Yamada S
AD  - Division of Pharmaceutical Sciences , Okayama University Graduate School of 
      Medicine, Dentistry and Pharmaceutical Sciences , 1-1-1, Tsushima-naka , Kita-ku, 
      Okayama 700-8530 , Japan.
AD  - Research Fellowship Division , Japan Society for the Promotion of Science , 
      Sumitomo-Ichibancho FS Bldg., 8 Ichibancho , Chiyoda-ku, Tokyo 102-8472 , Japan.
FAU - Kawasaki, Mayu
AU  - Kawasaki M
AD  - Graduate School of Integrated Pharmaceutical and Nutritional Sciences , 
      University of Shizuoka , 52-1 Yada , Suruga-ku, Shizuoka 422-8526 , Japan.
FAU - Fujihara, Michiko
AU  - Fujihara M
AD  - Division of Pharmaceutical Sciences , Okayama University Graduate School of 
      Medicine, Dentistry and Pharmaceutical Sciences , 1-1-1, Tsushima-naka , Kita-ku, 
      Okayama 700-8530 , Japan.
AD  - AIBIOS Co. Ltd. , Tri-Seven Roppongi 8F 7-7-7 Roppongi , Minato-ku, Tokyo 
      106-0032 Japan.
FAU - Watanabe, Masaki
AU  - Watanabe M
AD  - Division of Pharmaceutical Sciences , Okayama University Graduate School of 
      Medicine, Dentistry and Pharmaceutical Sciences , 1-1-1, Tsushima-naka , Kita-ku, 
      Okayama 700-8530 , Japan.
FAU - Takamura, Yuta
AU  - Takamura Y
AD  - Division of Pharmaceutical Sciences , Okayama University Graduate School of 
      Medicine, Dentistry and Pharmaceutical Sciences , 1-1-1, Tsushima-naka , Kita-ku, 
      Okayama 700-8530 , Japan.
FAU - Takioku, Maho
AU  - Takioku M
AD  - Division of Pharmaceutical Sciences , Okayama University Graduate School of 
      Medicine, Dentistry and Pharmaceutical Sciences , 1-1-1, Tsushima-naka , Kita-ku, 
      Okayama 700-8530 , Japan.
FAU - Nishioka, Hiromi
AU  - Nishioka H
AD  - Division of Pharmaceutical Sciences , Okayama University Graduate School of 
      Medicine, Dentistry and Pharmaceutical Sciences , 1-1-1, Tsushima-naka , Kita-ku, 
      Okayama 700-8530 , Japan.
FAU - Takeuchi, Yasuo
AU  - Takeuchi Y
AD  - Division of Pharmaceutical Sciences , Okayama University Graduate School of 
      Medicine, Dentistry and Pharmaceutical Sciences , 1-1-1, Tsushima-naka , Kita-ku, 
      Okayama 700-8530 , Japan.
FAU - Makishima, Makoto
AU  - Makishima M
AUID- ORCID: 0000-0002-4630-905X
AD  - Division of Biochemistry, Department of Biomedical Sciences , Nihon University 
      School of Medicine , 30-1 Oyaguchi-kamicho , Itabashi-ku, Tokyo 173-8610 , Japan.
FAU - Motoyama, Tomoharu
AU  - Motoyama T
AD  - Graduate School of Integrated Pharmaceutical and Nutritional Sciences , 
      University of Shizuoka , 52-1 Yada , Suruga-ku, Shizuoka 422-8526 , Japan.
FAU - Ito, Sohei
AU  - Ito S
AUID- ORCID: 0000-0002-9937-3100
AD  - Graduate School of Integrated Pharmaceutical and Nutritional Sciences , 
      University of Shizuoka , 52-1 Yada , Suruga-ku, Shizuoka 422-8526 , Japan.
FAU - Tokiwa, Hiroaki
AU  - Tokiwa H
AUID- ORCID: 0000-0002-3790-1799
FAU - Nakano, Shogo
AU  - Nakano S
AUID- ORCID: 0000-0002-6614-7158
AD  - Graduate School of Integrated Pharmaceutical and Nutritional Sciences , 
      University of Shizuoka , 52-1 Yada , Suruga-ku, Shizuoka 422-8526 , Japan.
FAU - Kakuta, Hiroki
AU  - Kakuta H
AUID- ORCID: 0000-0002-3633-8121
AD  - Division of Pharmaceutical Sciences , Okayama University Graduate School of 
      Medicine, Dentistry and Pharmaceutical Sciences , 1-1-1, Tsushima-naka , Kita-ku, 
      Okayama 700-8530 , Japan.
LA  - eng
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
DEP - 20190918
PL  - United States
TA  - J Med Chem
JT  - Journal of medicinal chemistry
JID - 9716531
RN  - 0 (Fluorescent Dyes)
RN  - 0 (Ligands)
RN  - 0 (Retinoid X Receptors)
RN  - 0 (Tetrahydronaphthalenes)
RN  - 0 (Umbelliferones)
SB  - IM
MH  - Binding, Competitive
MH  - Fluorescent Dyes/*chemistry
MH  - Genes, Reporter
MH  - Humans
MH  - Hydrophobic and Hydrophilic Interactions
MH  - Inhibitory Concentration 50
MH  - *Ligands
MH  - Protein Binding
MH  - Retinoid X Receptors/*agonists/genetics/metabolism
MH  - Tetrahydronaphthalenes/chemistry
MH  - Umbelliferones/*chemistry/metabolism
EDAT- 2019/09/05 06:00
MHDA- 2020/06/17 06:00
CRDT- 2019/09/05 06:00
PHST- 2019/09/05 06:00 [pubmed]
PHST- 2020/06/17 06:00 [medline]
PHST- 2019/09/05 06:00 [entrez]
AID - 10.1021/acs.jmedchem.9b00995 [doi]
PST - ppublish
SO  - J Med Chem. 2019 Oct 10;62(19):8809-8818. doi: 10.1021/acs.jmedchem.9b00995. Epub 
      2019 Sep 18.