Bridged Bicyclic Aromatic Compounds for Retinoid-X Receptor Homodimer Formation

摘要

The present invention provides a method for screening a substance for its ability to influence the formation of a retinoid X receptor homodimer, including mixing the substance with a solution containing the retinoid X receptor and measuring the presence of homodimer formation. Screening methods can be used to determine compounds that selectively activate homodimer formation and heterodimer formation. The invention also screens a substance for its effect on the ability of the retinoid X receptor homodimer to bind DNA, including measuring the effect of the compound on the ability of the homodimer to mix the substance with the homodimer and bind DNA. Provide a way to. As a result, the present invention provides a method of activating retinoid X receptor homodimer formation. Bridged bicyclic aromatic compounds provide compounds of formula (I) wherein R ¹ , R ² , R ³ , R ⁴ , R ⁵ and n are as defined herein. The compounds of the present invention are useful for regulating gene expression of retinoic acid receptors, vitamin D receptors and thyroid receptors. The invention also provides pharmaceutical compositions and methods for modulating gene expression.