(17.ALPHA.,20E)-17,20-[(1-Methoxyethylidene)bis(oxy)]-3-oxo-19-norpregna-4,20-diene-21-carboxylic Acid Methyl Ester (YK11) Is a Partial Agonist of the Androgen Receptor
-
- Kanno Yuichiro
- Faculty of Pharmaceutical Sciences, Toho University
-
- Hikosaka Ritsuko
- Faculty of Pharmaceutical Sciences, Toho University
-
- Zhang Shu-Yun
- Faculty of Pharmaceutical Sciences, Toho University
-
- Inoue Yoshimi
- Faculty of Pharmaceutical Sciences, Toho University
-
- Nakahama Takayuki
- Faculty of Pharmaceutical Sciences, Toho University
-
- Kato Keisuke
- Faculty of Pharmaceutical Sciences, Toho University
-
- Yamaguchi Akemi
- Department of Chemical and Biological Engineering, Ariake National College of Technology
-
- Tominaga Nobuaki
- Department of Chemical and Biological Engineering, Ariake National College of Technology
-
- Kohra Shinya
- Faculty of Environmental Studies, Nagasaki University
-
- Arizono Koji
- Faculty of Environmental and Symbiotic Sciences, Prefectural University of Kumamoto
-
- Inouye Yoshio
- Faculty of Pharmaceutical Sciences, Toho University
Bibliographic Information
- Other Title
-
- (17α,20E)-17,20-〔(1-methoxyethylidene)bis(oxy)〕-3-oxo-19-norpregna-4,20-diene-21-carboxylic acid methyl ester (YK11) is a partial agonist of the androgen receptor
- 17 a 20E 17 20 1 methoxyethylidene bis oxy 3 oxo 19 norpregna 4 20 diene 21 carboxylic acid methyl ester YK11 is a partial agonist of the androgen receptor
- (17α,20E)-17,20-[(1-methoxyethylidene)bis(oxy)]-3-oxo-19-norpregna-4,20-diene-21-carboxylic acid methyl ester (YK11) is a partial agonist of the androgen receptor
Search this article
Description
A novel steroid compound, (17α,20E)-17,20-[(1-methoxyethylidene)bis(oxy)]-3-oxo-19-norpregna-4,20-diene-21-carboxylic acid methyl ester (YK11), was found to be a partial agonist of the androgen receptor (AR) in an androgen responsive element (ARE)-luciferase reporter assay. YK11 accelerates nuclear translocation of AR. Furthermore, YK11 does not induce amino/carboxyl-terminal (N/C) interaction and prevents 5-α-dihydrotestosterone (DHT)-mediated N/C interaction. Thus, YK11 activates AR without causing N/C interaction, which may in turn be responsible for the partially agonistic nature of YK11 observed in the ARE-luciferase reporter system. YK11 acts as a gene-selective agonist of AR in MDA-MB 453 cells. The effect of YK11 on gene expression relative to that of androgen agonist varies depending on the gene context. YK11 activated the reporter gene by inducing the translocation of the AR into the nuclear compartment, where its amino-terminal domain (NTD) functions as a constitutive activator of AR target genes. Our results suggest that YK11 might act as selective androgen receptor modulator (SARM).
Journal
-
- Biological and Pharmaceutical Bulletin
-
Biological and Pharmaceutical Bulletin 34 (3), 318-323, 2011
The Pharmaceutical Society of Japan
- Tweet
Details 詳細情報について
-
- CRID
- 1390001204627698944
-
- NII Article ID
- 130000657806
-
- NII Book ID
- AA10885497
-
- ISSN
- 13475215
- 09186158
-
- NDL BIB ID
- 10989976
-
- PubMed
- 21372378
-
- Text Lang
- en
-
- Data Source
-
- JaLC
- NDL Search
- Crossref
- CiNii Articles
- OpenAIRE
-
- Abstract License Flag
- Disallowed