IP Library Granted Patent US 9,421,197
Granted Patent B2
US 9,421,197 · App. 14/444,509 · Granted Aug 23, 2016

Methods of generating hyper INOS expressing cells and uses thereof

Inventors: Kurt Q. Lu (Cleveland Heights, OH); Kevin D. Cooper (Moreland Hills, OH)
Assignee: Case Western Reserve University
A61K31/4439A61K31/426A61K38/00A61K39/3955A61K39/39533A61K45/06C12N5/0645C12N2500/36C12N2501/23C12N2501/385
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Quick Facts
Patent No.
US 9,421,197
App. No.
14/444,509
Granted
Aug 23, 2016
Kind
B2
Abstract

A method of generating a hyper iNOS expressing cell includes administering to a myeloid derived cell an amount of a PPARγ agonist and an IL-6/STAT3 signaling pathway antagonist effective to substantially inhibit STAT3 activation in the cell and administering an inflammatory insult to the cell to stimulate hyper iNOS expression from the cell.

Claims (12)

1. A method of treating skin cancer or a skin tumor in a subject comprising:

administering an amount of a PPARy agonist and an IL-6/STAT3 signaling

pathway antagonist to the subject effective to substantially inhibit STAT3 activation in the macrophages of the subject; and

administering an amount of an inflammatory or damaging insult to the skin cancer or skin tumor of the subject effective to induce hyper iNOS expression of the macrophages that are in or about the periphery of the skin cancer or skin tumor.

2. The method of claim 1 , the insult being administered directly to or about the periphery of the skin cancer or skin tumor.

3. The method of claim 1 , the insult comprising at least one of trauma, physical stress, chemical stress, biological stress, or radiation.

4. The method of claim 1 , the PPARy agonist comprising a thiazolidinedione or a derivative thereof.

5. The method of claim 1 , the PPARy agonist comprising at least one compound or a pharmaceutically salt thereof selected from the group consisting of: (+)-5[[4-[(3,4-dihydro-6-hydroxy-2,5,7,8-tetramethyl-2H-1-benzopyran-2-yl)m ethoxy]phenyl]methyl]-2,4thiazolidinedione; 5-[4-[2-(5-ethylpyridin-2-yl)ethoxyl]benzyl]thiazolidine-2,4-dione; 5-[4-[(l methylcyclohexyl)methoxy]benzyl]thiazolidine-2,4-dione; (ciglitazone); 4-(2-naphthylmethyl)-1,2,3,5-oxathiadiazole-2-oxide; 5-[4-[2-[(N-(benzoxazol-2-yl)-Nmethylamino]ethoxy]benzyl]-5-methlthiazolidine-2,4-dione; 5-[4-[2-[2,4dioxo-5-phenylthiazolidine-3-yl)ethoxy]benzyl]thiazolidine-2,4-dione; 5-[4-[2-[(N-methyl-N(phenoxycarbonyl)amino]ethoxy]benzyl]thiazolidine-2,4-dione; 5-[4-[2-phenoxyethoxy)benzyl]thiazolidine-2,4-dione; 5-[4-[2-(4-chorophenyl)ethylsulfonyl]benzyl]thiazolidine-2,4-dione; 5-[4-[3-(5-methyl-2-phenyloxazol-4-yl)propionyl]benzyl]thiazolidine-2,4-dione; 5-[[4-(3-hydroxy-1-methylcyclohexyl)methoxy]benzyl]thiazolidine-2,4-dione; 5-[4-[2-(5-methy 1-2-phenyloxazol-4-yl)ethoxyl]benzyl]thiazolidine-2,4-dione; 5-[(2-benzyl-2,3-dihydrobenzopyran)-5-ylmethyl]thiazolidine-2,4-dione; 5-[[2-(2-42-naphthylmethyl)benzoxazol]-5-ylmethyl]thiazolidine-2,4-dione; 5-[4-[2-(3-phenylureido)ethoxyl]benzyl]thiazolidine-2,4-dione; 5-[4-[2-(N-benzoxazol-2-yl)-Nmetholamino]ethoxy]benzyl]thiazolidine-2,4-dione; 5-[4-[3-(5-methyl-2-phenyloxazol-4-yl)propionyl]benzyl]thiazolidine-2,4-dione; 5-[2-(5-methyl-2-phenyloxazol-4-ylmethyl)benzofuran-5-ylmethyl]oxazolidine-2,4-dione; 5-[4-[2-(N-methyl-N-(2-pyridyl)amino]ethoxy]benzyl]thiazolidine-2,4-dione; and 5-[4-[2-(N-(benzoxazol-2-yl)-Nmethylamino]ethoxy]benzyl]oxazolidine-2,4-dione.

6. The method of claim 1 , wherein the IL-6/STAT3 signaling pathway antagonist comprises at least one of an antibody, peptide, or small molecule.

7. The method of claim 1 , wherein the IL-6/STAT3 signaling pathway antagonist is an HMG CoA reductase inhibitor.

8. The method of claim 1 , wherein the IL-6/STAT3 signaling pathway antagonist is a STAT3 inhibitor.

9. The method of claim 1 , the PPARy agonist being administered to the skin cancer in a topical formulation.

Assignments (2)
CONFIRMATORY LICENSE Recorded Mar 14, 2018
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 045588/0165 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 7, 2016
From: LU, KURT Q; COOPER, KEVIN D
To: CASE WESTERN RESERVE UNIVERSITY
Reel/Frame 039102/0562 →
Continuity (6)
Continuation 13780503 · Feb 28, 2013
Continuation 13578785
Provisional Application 61303871 · Feb 12, 2010
Provisional Application 61434151 · Jan 19, 2011
Provisional Application 61320879 · Apr 5, 2010
Related Publication 20140335105A1 · Nov 13, 2014