IP Library Granted Patent US 10,561,636
Granted Patent B2
US 10,561,636 · App. 16/340,352 · Granted Feb 18, 2020

Methods of treating disorders with glycosylation defective proteins

Inventors: Kumar N. Alagramam (Cleveland, OH); Suhasini Gopal (Cleveland, OH)
Assignee: CASE WESTERN RESERVE UNIVERSITY
A61K31/357A61K31/365
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Quick Facts
Patent No.
US 10,561,636
App. No.
16/340,352
Granted
Feb 18, 2020
Kind
B2
Abstract

A method of treating a glycosylation-defective protein associated disease or disorder in a subject, the method includes administering to the subject a therapeutically effective amount of a Sarco/ER ATPase (SERCA) inhibitor.

Claims (25)

1. A method of treating a glycosylation-defective protein associated disease or disorder in a subject in need thereof, the method comprising:

administering to the subject a therapeutically effective amount of a Sarco/ER ATPase (SERCA) inhibitor.

2. The method of claim 1 , the SERCA inhibitor selected from the group consisting of Artemisinin, Artesunate (Arts), thapsigargin, mipsagargin, DBHQ (2,5-di-tert-butylhydroquinone), Saikosaponin-d (Ssd), SBF-1, ruthenium red, curcumin, F36, gingerol, paxilline, cyclopiazonic acid, sHA14-1, CXL017, and analogs thereof.

3. The method of claim 2 , the SERCA inhibitor comprising Artesunate (Arts).

4. The method of claim 1 , wherein the therapeutically effective amount is the amount required to increase cytosolic calcium levels and perturb ER in cells of the subjects.

5. The method of claim 1 , wherein the therapeutically effective amount is an amount effective to potentiate ER stress and unfolded protein response (UPR) in cells of the subjects.

6. The method of claim 1 , the glycosylation-defective protein associated disease or disorder is a human clarin-1 protein (hCLRN1) defect related disease or disorder.

7. The method of claim 6 , the hCLRN1 defect related disease or disorder comprising a hCLRN1 N48k missense mutation related disease or disorder.

8. The method of claim 7 , the hCLRN1 N48K missense mutation related disease or disorder comprising Usher syndrome type III (USH3).

9. A method of treating a sensory deficit in a subject associated with a mutation of the human clarin-1 protein hCLRN1 protein, the method comprising:

administering to the subject a therapeutically effective amount of a Sarco/ER ATPase (SERCA) inhibitor.

10. The method of claim 9 , the sensory deficit comprising hearing loss.

11. The method of claim 10 , the therapeutically effective amount comprising an amount effective to promote hCLRN1 N48K localization to hair bundles of a hair cell.

12. The method of claim 9 , the SERCA inhibitor selected from the group consisting of Artemisinin, Artesunate (Arts), thapsigargin, mipsagargin, DBHQ (2,5-di-tert-butylhydroquinone), Saikosaponin-d (Ssd), SBF-1, ruthenium red, curcumin, F36, gingerol, paxilline, cyclopiazonic acid, sHA14-1, CXL017, and analogs thereof.

13. The method of claim 9 , the SERCA inhibitor comprising Artesunate (Arts).

14. The method of claim 9 , wherein the SERCA inhibitor is administered prior to sensory deficit in a subject.

15. The method of claim 9 , the sensory deficit associated with the N48K destabilizing missense mutation in the human clarin-1 protein (hCLRN1 N48k ).

16. A method of treating Usher syndrome type III (USH3) in a subject, the method comprising:

administering to the subject a therapeutically effective amount of a Sarco/ER ATPase (SERCA) inhibitor.

17. The method of claim 16 , wherein USH3 is associated with a human clarin-1 protein (hCLRN1) missense mutation.

18. The method of claim 17 , the hCLRN1 missense mutation comprising hCLRN1 N48K .

19. The method of claim 16 , the SERCA inhibitor selected from the group consisting of Artemisinin, Artesunate (Arts), thapsigargin, mipsagargin, DBHQ (2,5-di-tert-butylhydroquinone), Saikosaponin-d (Ssd), SBF-1, ruthenium red, curcumin, F36, gingerol, paxilline, cyclopiazonic acid, sHA14-1, CXL017, and analogs thereof.

20. The method of claim 19 , the SERCA inhibitor comprising Artesunate (Arts).

21. The method of claim 16 , the therapeutically effective amount comprising an amount effective to promote hCLRN1 N48K localization to hair bundles of a hair cell.

22. The method of claim 16 , wherein the SERCA inhibitor is administered prior to sensory deficit in the USH3 subject.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 5, 2019
From: KUMAR, ALAGRAMAM N.; GOPAL RAMANUJAM, SUHASINI
To: CASE WESTERN RESERVE UNIVERSITY
Reel/Frame 050917/0848 →
Continuity (2)
Provisional Application 62405351 · Oct 7, 2016
Related Publication 20190231741A1 · Aug 1, 2019