C - Chemistry – Metallurgy – 12 – Q
Patent
C - Chemistry, Metallurgy
12
Q
C12Q 1/68 (2006.01) A61K 31/19 (2006.01) A61K 31/335 (2006.01) A61K 31/36 (2006.01) A61K 31/38 (2006.01) C07C 63/49 (2006.01) C07C 63/66 (2006.01) C07C 65/36 (2006.01) C07C 69/738 (2006.01) C07C 69/76 (2006.01) C07D 317/30 (2006.01) C07D 319/06 (2006.01) C07D 327/04 (2006.01) C07D 333/38 (2006.01) C07D 339/06 (2006.01) C07D 339/08 (2006.01) C07D 409/04 (2006.01) C07K 14/705 (2006.01) G01N 33/566 (2006.01) G01N 33/68 (2006.01) G01N 33/74 (2006.01)
Patent
CA 2149882
2149882 9412880 PCTABS00032 The invention provides a method of screening a substance for the ability to affect the formation of a retinoid X receptor homodimer comprising combining the substance and a solution containing retinoid X receptors and determining the presence of homodimer formation. The screening method can be used to determine compounds which selectively activate homodimer formation and heterodimer formation. Also provided is a method of screening a substance for an effect on a retinoid X receptor homodimer's ability to bind DNA comprising combining the substance with the homodimer and determining the effect of the compound on the homodimer's ability to bind DNA. Finally, the invention provides methods of activating retinoid X receptor homodimer formation. Bridged bicyclic aromatic compounds are provided having structure (I); wherein R1, R2, R3, R4, R5 and n are as defined herein. The compounds are useful for modulating gene expression of retinoic acid receptors, vitamin D receptors and thyroid receptors. Pharmaceutical compositions and methods for modulating gene expression are provided as well.
Cameron James F.
Dawson Marcia I.
Hobbs Peter D.
Jong Ling
Lehmann Jurgen M.
Ligand Pharmaceuticals Inc.
Sim & Mcburney
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