IP Library Granted Patent US 9,845,512
Granted Patent B2
US 9,845,512 · App. 12/985,232 · Granted Dec 19, 2017

Screening assay employing Dex and GDF8

Inventor: Todd M. Kinsella (Redwood City, CA)
Assignee: RIGEL PHARMACEUTICALS, INC.
C12Q1/6897A61K31/573A61K38/1841A61K45/06G01N2333/71G01N2333/723G01N2500/10
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Quick Facts
Patent No.
US 9,845,512
App. No.
12/985,232
Granted
Dec 19, 2017
Kind
B2
Abstract

Certain aspects of this disclosure relate to a method that comprises contacting a mammalian cell with a glucocorticoid receptor ligand and a myostatin receptor ligand, thereby activating the glucocorticoid receptor and said myostatin receptor. A screening assay employing the same is also provided.

Claims (21)

1. A method comprising:

contacting a mammalian cell comprising a glucocorticoid receptor, a myostatin receptor and a recombinant nucleic acid comprising an atrogen promoter that is at least 95% identical to a wild type MURF-1 or MAFbx promoter and operably linked to a coding sequence encoding a reporter protein, with a ligand that activates the glucocorticoid receptor and a ligand that is at least 90% identical to a wild-type mammalian GDF8 and activates the myostatin receptor, thereby activating said atrogen promoter and inducing expression of said reporter protein.

2. The method of claim 1 , wherein said contacting initiates an atrophy response by said mammalian cell.

3. The method of claim 1 , wherein said contacting is done by contacting said ligand that activates the glucocorticoid receptor and said ligand that activates the myostatin receptor with a cultured cell in vitro.

4. The method of claim 3 , wherein said ligand that activates the glucocorticoid receptor is contacted with said mammalian cell at a concentration in the range of 0.1 μM to 100 μM.

5. The method of claim 3 , wherein said ligand that activates the myostatin receptor is contacted with said mammalian cell at a concentration of 1 ng/mL to 1000 ng/mL.

6. The method of claim 1 , wherein said contacting is done by administering said ligand that activates the glucocorticoid receptor and said ligand that activates the myostatin receptor to a mammal.

7. The method of claim 1 , wherein said ligand that activates the glucocorticoid receptor and said ligand that activates the myostatin receptor are contacted with said mammalian cell simultaneously.

8. The method of claim 1 , wherein said ligand that activates the glucocorticoid receptor and said ligand that activates the myostatin receptor are contacted with said mammalian cell at different times.

9. The method of claim 1 , wherein said ligand that activates the glucocorticoid receptor is dexamethasone.

10. The method of claim 1 , wherein said ligand that activates the myostatin receptor comprises an amino acid sequence that is at least 95% identical to a wild-type GDF8.

11. The method of claim 1 , wherein said ligand that activates the myostatin receptor is GDF8.

12. The method of claim 1 , wherein said atrogen promoter is identical to a wild type MURF-1 or MAFbx promoter.

13. The method of claim 1 , wherein the contacting is done in the presence of a candidate agent; and the method further comprises measuring production of the reporter protein.

14. The method of claim 13 , wherein the method further comprises determining if said candidate agent alters cell phenotype of said cell.

15. The method of claim 14 , wherein said cell phenotype is a muscle atrophy phenotype.

16. The method of claim 13 , wherein said contacting is done by contacting said candidate agent with a cultured cell in vitro; and the method further comprises determining a muscle atrophy phenotype in the cultured cell.

17. The method claim 13 , wherein said contacting is done by administering said candidate agent to a mammal; and the method further comprises determining a muscle atrophy phenotype in muscle tissue of the mammal.

18. The method of claim 17 , wherein said determining a muscle atrophy phenotype comprises measuring muscle mass.

19. The method of claim 17 , wherein said mammal is a rat.

20. The method of claim 13 , wherein said candidate agent is a siRNA.

Assignments (2)
SECURITY INTEREST Recorded Aug 25, 2022
From: RIGEL PHARMACEUTICALS, INC.
To: MIDCAP FINANCIAL TRUST
Reel/Frame 061327/0712 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 25, 2011
From: KINSELLA, TODD M.
To: RIGEL PHARMACEUTICALS, INC.
Reel/Frame 025866/0984 →
Continuity (2)
Provisional Application 61295631 · Jan 15, 2010
Related Publication 20110177001A1 · Jul 21, 2011