.

Pharmaceutical Business Intelligence

  • Anticipate P&T budget requirements
  • Evaluate market entry opportunities
  • Find generic sources and suppliers
  • Predict branded drug patent expiration

► Plans and Pricing

Upgrade to enjoy subscriber-only features like email alerts and data export. See the Plans and Pricing

DrugPatentWatch Database Preview

Details for Patent: 5,824,484

« Back to Dashboard

Details for Patent: 5,824,484

Title: RXR homodimer formation
Abstract:The invention provides a method of screening a substance for the ability to effect 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. 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. A method of inhibiting an activity of a retinoid X receptor heterodimer comprising increasing the formation of a retinoid X receptor homodimer, thereby preventing the retinoid X receptor from forming a heterodimer and preventing the resulting heterodimer activity is also provided. A method of inhibiting an activity of a retinoid X receptor homodimer is also provided. A method of determining an increased probability of a pathology associated with retinoid X receptor homodimer formation and treating such pathology are further provided. In addition, a method of screening a response element for binding with a retinoid X receptor homodimer is provided. Finally, the invention provides methods of activating retinoid X receptor homodimer formation.
Inventor(s): Pfahl; Magnus (Solana Beach, CA), Zhang; Xiao-kun (La Jolla, CA), Lehmann; Jurgen M. (Solana Beach, CA), Dawson; Marcia I. (Menlo Park, CA), Cameron; James F. (Palo Alto, CA), Hobbs; Peter D. (Moss Beach, CA), Jong; Ling (Sunnyvale, CA)
Assignee: La Jolla Cancer Research Foundation (La Jolla, CA)
Filing Date:Jan 22, 1996
Application Number:08/589,528
Claims:1. A method of inhibiting an activity of a retinoid X receptor heterodimer comprising inducing the formation of a retinoid X receptor homodimer, thereby inhibiting the retinoid X receptor from forming a heterodimer and inhibiting the resulting heterodimer activity.

2. The method of claim 1, wherein the activity is the activation or repression of transcription.

3. The method of claim 1, wherein the retinoid X receptor heterodimer is thyroid hormone receptor and retinoid X receptor.

4. A method of increasing the transcription of a gene activated by a retinoid X receptor (RXR) homodimer in a cells comprising contacting the cell with an amount of a synthetic compound having the structural formula ##STR5## which increases the formation of RXR homodimers, thereby increasing the transcription of a gene activated by an RXR homodimer.

5. A method of increasing the transcription of a gene activated by a retinoid X receptor (RXR) homodimer in a cell, comprising contacting the cell with an amount of a synthetic compound having the structural formula ##STR6## which increases the formation of RXR homodimers, thereby increasing the transcription of a gene activated by an RXR homodimer.

6. A method of increasing the transcription of a gene activated by a retinoid X receptor (RXR) homodimer in a cell, comprising contacting the cell with an amount of a synthetic compound having the structural formula ##STR7## wherein R, R.sup.1 is selected from the group consisting of SCH.sub.2 CH.sub.2 CH.sub.2 S SCH.sub.2 CH.sub.2 S, OCH.sub.2 CH.sub.2 S and OCH.sub.2 CH.sub.2 CH.sub.2 O, wherein said synthetic compound increases the formation of RXR homodimers, thereby increasing the transcription of a gene activated by an RXR homodimer.

7. A method of selectively activating retinoid X receptor (RXR) homodimer formation in a cell comprising adding to the cell a homodimer formation specific ligand, thereby selectively activating RXR homodimer formation in the cell.

8. The method of claim 7, wherein the homodimer formation specific ligand has the structural formula ##STR8##

9. A method of selectively activating retinoid X receptor (RXR) homodimer formation in a cell, comprising adding to the cell a homodimer formation specific ligand having the structural formula ##STR9## thereby selectively activating RXR homodimer formation in the cell.

10. A method of selectively activating retinoid X receptor (RXR) homodimer formation in a cell, comprising adding to the cell a homodimer formation specific ligand having the structural formula ##STR10## wherein R, R.sup.1 is selected from the group consisting of SCH.sub.2 CH.sub.2 CH.sub.2 S, SCH.sub.2 CH.sub.2 S, OCH.sub.2 CH.sub.2 S and OCH.sub.2 CH.sub.2 CH.sub.2 O, thereby selectively activating RXR homodimer formation in the cell.

11. A method of increasing retinoid X receptor (RXR) homodimer formation in a cell, comprising contacting the cell with 9-cis-RA, thereby increasing RXR homodimer formation.
« Back to Dashboard

For more information try a trial or see the database preview and plans and pricing

How are People Using DrugPatentWatch?

Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verifification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.

`abc