IP Library Granted Patent US 11,865,103
Granted Patent B2
US 11,865,103 · App. 17/468,274 · Granted Jan 9, 2024

Methods of treating disorders associated with glycosylation defective proteins

Inventors: Alagramam N. Kumar (Cleveland, OH); Suhasini Gopal Ramanujam (Cleveland, OH)
Assignee: CASE WESTERN RESERVE UNIVERSITY
A61K31/357A61K31/343A61P27/16
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Quick Facts
Patent No.
US 11,865,103
App. No.
17/468,274
Granted
Jan 9, 2024
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 (9)

1. A method of liberating deleterious glycosylation-defective misfolded proteins that accumulate in endoplasmic reticulum (ER) of a subject's cells that are associated with and/or causative of a 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, wherein the SERCA inhibitor induces unconventional secretory pathway transport of aggregated glycosylation-defective protein from endoplasmic reticulum of cells of the subject.

2. The method of claim 1 , wherein the SERCA inhibitor reduces endoplasmic reticulum luminal calcium levels.

3. The method of claim 1 , wherein the SERCA inhibitor induces activation of the GRASP55 cargo dependent unconventional secretory pathway (GCUSP).

4. 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.

5. The method of claim 1 , the SERCA inhibitor comprising Artesunate (Arts).

6. 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 subject.

7. 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 subject.

8. The method of claim 1 , the SERCA inhibitor being administered to the subject by at least one of ophthalmic, topical, parenteral, subcutaneous, intravenous, intraarticular, intrathecal, intramuscular, intraperitoneal, intradermal, transdermal, buccal, oromucosal, oral, or inhalation administration.

Assignments (1)
CONFIRMATORY LICENSE Recorded Jan 31, 2024
From: CASE WESTERN RESERVE UNIVERSITY
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 066385/0662 →
Continuity (4)
Continuation 16793861 · Feb 18, 2020
Continuation In Part 16340352
Provisional Application 62405351 · Oct 7, 2016
Related Publication 20220168269A1 · Jun 2, 2022