A novel nuclear receptor ligand, digoxigenin, is a selective antagonist of liver-X-receptors

Haruka Oishi; Yousuke Takaoka; Tomoko Nishimaki-Mogami; Hiroaki Saito; Minoru Ueda

doi:10.1246/cl.161071

A novel nuclear receptor ligand, digoxigenin, is a selective antagonist of liver-X-receptors

Haruka Oishi, Yousuke Takaoka, Tomoko Nishimaki-Mogami, Hiroaki Saito, Minoru Ueda

SCI - Chemistry

Research output: Contribution to journal › Article › peer-review

1 Citation (Scopus)

Abstract

Recent progress in chemical biology of natural products has revealed the multiligandable nature, and exploration of new natural product targets often leads to the discovery of novel drug leads. We focused on digoxigenin (1), which is an aglycone of the steroid glycoside digoxin. The in vitro binding assay using the ligand binding domain of nuclear receptors indicated that 1 is a potential antagonist of liver-X-receptors, a result that was supported by an in silico docking study.

Original language	English
Pages (from-to)	313-314
Number of pages	2
Journal	Chemistry Letters
Volume	46
Issue number	3
DOIs	https://doi.org/10.1246/cl.161071
Publication status	Published - 2017

Keywords

Drug discovery
Natural products
Nuclear receptor

ASJC Scopus subject areas

Chemistry(all)

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10.1246/cl.161071

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title = "A novel nuclear receptor ligand, digoxigenin, is a selective antagonist of liver-X-receptors",

abstract = "Recent progress in chemical biology of natural products has revealed the multiligandable nature, and exploration of new natural product targets often leads to the discovery of novel drug leads. We focused on digoxigenin (1), which is an aglycone of the steroid glycoside digoxin. The in vitro binding assay using the ligand binding domain of nuclear receptors indicated that 1 is a potential antagonist of liver-X-receptors, a result that was supported by an in silico docking study.",

keywords = "Drug discovery, Natural products, Nuclear receptor",

author = "Haruka Oishi and Yousuke Takaoka and Tomoko Nishimaki-Mogami and Hiroaki Saito and Minoru Ueda",

note = "Funding Information: We thank Prof. S. Nishizawa, Dr. Y. Sato, and Mr. T. Sato (Tohoku Univ.) for fluorescent anisotropy experiments, and Dr. S. Tamura (Iwate Medical University) for useful discussion. This work was supported in part by a Grant-in-Aid for Scientific Research (No. 23102012) from Innovative Areas {"}Chemical Biology of Natural Products{"} to M.U. from MEXT, Japan. Publisher Copyright: {\textcopyright} 2017 The Chemical Society of Japan.",

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doi = "10.1246/cl.161071",

language = "English",

volume = "46",

pages = "313--314",

journal = "Chemistry Letters",

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T1 - A novel nuclear receptor ligand, digoxigenin, is a selective antagonist of liver-X-receptors

AU - Oishi, Haruka

AU - Takaoka, Yousuke

AU - Nishimaki-Mogami, Tomoko

AU - Saito, Hiroaki

AU - Ueda, Minoru

N1 - Funding Information: We thank Prof. S. Nishizawa, Dr. Y. Sato, and Mr. T. Sato (Tohoku Univ.) for fluorescent anisotropy experiments, and Dr. S. Tamura (Iwate Medical University) for useful discussion. This work was supported in part by a Grant-in-Aid for Scientific Research (No. 23102012) from Innovative Areas "Chemical Biology of Natural Products" to M.U. from MEXT, Japan. Publisher Copyright: © 2017 The Chemical Society of Japan.

PY - 2017

Y1 - 2017

N2 - Recent progress in chemical biology of natural products has revealed the multiligandable nature, and exploration of new natural product targets often leads to the discovery of novel drug leads. We focused on digoxigenin (1), which is an aglycone of the steroid glycoside digoxin. The in vitro binding assay using the ligand binding domain of nuclear receptors indicated that 1 is a potential antagonist of liver-X-receptors, a result that was supported by an in silico docking study.

AB - Recent progress in chemical biology of natural products has revealed the multiligandable nature, and exploration of new natural product targets often leads to the discovery of novel drug leads. We focused on digoxigenin (1), which is an aglycone of the steroid glycoside digoxin. The in vitro binding assay using the ligand binding domain of nuclear receptors indicated that 1 is a potential antagonist of liver-X-receptors, a result that was supported by an in silico docking study.

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KW - Nuclear receptor

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JO - Chemistry Letters

JF - Chemistry Letters

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ER -

A novel nuclear receptor ligand, digoxigenin, is a selective antagonist of liver-X-receptors

Abstract

Keywords

ASJC Scopus subject areas

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