Title:
FLUORESCENT LIGAND FOR RETINOID X RECEPTOR, AND APPLICATION THEREOF
Document Type and Number:
WIPO Patent Application WO/2017/094838
Kind Code:
A1
Abstract:
By using a fluorescent ligand for a retinoid X receptor (RXR), said ligand being indicated by one of the following formulas (1)-(3), an evaluative test of ability to bind with RXR can be easily performed. (In the formulas, R1 is methyl, alkoxy, or styryl, R2 is hydroxy, alkoxy, or alkylamino, A is N or CH, B is NH or O, R3 is isopropyl or tertiary butyl, and R4 is isopropyl or isobutyl.)
Inventors:
KAKUTA HIROKI (JP)
YAMADA SHOYA (JP)
WATANABE MASAKI (JP)
YAMADA SHOYA (JP)
WATANABE MASAKI (JP)
Application Number:
PCT/JP2016/085729
Publication Date:
June 08, 2017
Filing Date:
December 01, 2016
Export Citation:
Assignee:
NAT UNIV CORP OKAYAMA UNIV (JP)
International Classes:
C07D213/80; A61K31/352; A61K31/44; A61K31/4433; A61K31/4704; A61K31/4709; A61P3/00; A61P3/10; A61P7/00; A61P25/16; A61P25/28; A61P35/00; A61P43/00; C07D215/54; C07D311/16; C07D401/12; C07D405/12; G01N33/15; G01N33/50
Domestic Patent References:
| WO2006103813A1 | 2006-10-05 |
Foreign References:
| JPH02297045A | 1990-12-07 |
Other References:
KOICHI SAITO ET AL: ""Biotechnology for 5-15 A Analysis of Biological Effects of Endocrine 1-4 Disrupting Chemicals on Wildlife Using Nuclear Hormone Receptor Superfamily", JOURNAL OF ENVIRONMENTAL BIOTECHNOLOGY, vol. 3, 2003, pages 3 - 13
OZERS, M. S. ET AL.: "Analysis of Ligand-Dependent Recruitment of Coactivator Peptides to Estrogen Receptor Using Fluorescence Polarization", MOLECULAR ENDOCRINOLOGY, vol. 19, no. 1, January 2005 (2005-01-01), pages 25 - 34, XP055599442
YAMADA, S. ET AL.: "Fluorescent retinoid X receptor ligands for fluorescence polarization assay", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, vol. 20, 2010, pages 5143 - 5146, XP027207944
OHSAWA, F. ET AL.: "Mechanism of Retinoid X Receptor Partial Agonistic Action of 1-(3, 5, 5, 8, 8-Pentamethyl-5, 6, 7, 8-tetrahydro-2-naphthyl)-1H-b enzotriazole-5-carboxylic Acid and Structural Development To Increase Potency", JOURNAL OF MEDICINAL CHEMISTRY, vol. 56, 2013, pages 1865 - 1877, XP055157660, DOI: doi:10.1021/jm400033f
WOODS, L. L. ET AL.: "Coumarin-3-carboxylic Acids", THE JOURNAL OF ORGANIC CHEMISTRY, vol. 30, pages 312 - 313, XP000983898, DOI: doi:10.1021/jo01012a517
SHERMAN, W. R. ET AL.: "Fluorescence of Substituted 7-Hydroxycoumarins", ANALYTICAL CHEMISTRY, vol. 40, no. 4, April 1968 (1968-04-01), pages 803 - 805, XP055599446
OZERS, M. S. ET AL.: "Analysis of Ligand-Dependent Recruitment of Coactivator Peptides to Estrogen Receptor Using Fluorescence Polarization", MOLECULAR ENDOCRINOLOGY, vol. 19, no. 1, January 2005 (2005-01-01), pages 25 - 34, XP055599442
YAMADA, S. ET AL.: "Fluorescent retinoid X receptor ligands for fluorescence polarization assay", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, vol. 20, 2010, pages 5143 - 5146, XP027207944
OHSAWA, F. ET AL.: "Mechanism of Retinoid X Receptor Partial Agonistic Action of 1-(3, 5, 5, 8, 8-Pentamethyl-5, 6, 7, 8-tetrahydro-2-naphthyl)-1H-b enzotriazole-5-carboxylic Acid and Structural Development To Increase Potency", JOURNAL OF MEDICINAL CHEMISTRY, vol. 56, 2013, pages 1865 - 1877, XP055157660, DOI: doi:10.1021/jm400033f
WOODS, L. L. ET AL.: "Coumarin-3-carboxylic Acids", THE JOURNAL OF ORGANIC CHEMISTRY, vol. 30, pages 312 - 313, XP000983898, DOI: doi:10.1021/jo01012a517
SHERMAN, W. R. ET AL.: "Fluorescence of Substituted 7-Hydroxycoumarins", ANALYTICAL CHEMISTRY, vol. 40, no. 4, April 1968 (1968-04-01), pages 803 - 805, XP055599446
Attorney, Agent or Firm:
SETOUCHI INTERNATIONAL PATENT FIRM (JP)
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