Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
2053090 | FEBS Letters | 2005 | 6 Pages |
Abstract
Liver X receptors (LXRs) α and β share considerable sequence homology and several functions, respond to the same endogenous and synthetic ligands, and play critical roles in maintaining lipid homeostasis. In this study, liverwort-derived riccardin C (RC) and F (RF) were identified as an LXRα agonist/LXRβ antagonist and an LXRα antagonist, respectively. RC and RF bound to LXRs, but had different abilities to recruit a coactivator and thereby induce transactivation. Despite its unique subtype-selective activity, RC enhanced ABCA1 and ABCG1 expression and cellular cholesterol efflux in THP-1 cells. RC may provide a novel tool for identifying subtype-function and drug development.
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Authors
Norimasa Tamehiro, Yoji Sato, Takuo Suzuki, Toshihiro Hashimoto, Yoshinori Asakawa, Shinji Yokoyama, Tohru Kawanishi, Yasuo Ohno, Kazuhide Inoue, Taku Nagao, Tomoko Nishimaki-Mogami,