Protein Arginine Deiminase Inhibitors as a Novel Therapeutic Strategy for Rheumatoid Arthritis, Cancer and Other Human Diseases

Description:

Reference #:  00812

Potential Applications:

 

These Protein Arginine Deiminase Inhibitors aid in the treatment of cancer and arthritis.

 

Advantages and Benefits:

 

·      The most potent inhibitors of PAD4 activity known to date
·      Have in vivo applicability
·      Exhibit cytotoxicity towards cells of cancerous lineage without affecting non-cancerous cells
·      Trigger cell differentiation into non-cancerous granulocytes 

 

Background:

 

Cancer is a leading cause of mortality worldwide, killing nearly 8 million people every year and costing close to $125 billion annually. An estimated 1.5 million adults in the U.S. suffer from rheumatoid arthritis. Both diseases negatively affect the quality of life of the patient and burden caretakers. New and improved treatment options are needed that effectively treat these costly diseases.

 

Invention Description:

 

This technology identifies two potent, irreversible inactivators targeting Protein Arginine Deiminases (PADs), a family of enzymes that are believed to play roles in various human diseases, including rheumatoid arthritis (RA) and cancer.  These second generation haloacetamidine-based PAD inhibitors contain either a fluoro- or a chloro-acetamidine warhead in place of the guanidinium moiety of arginine containing substrates.  These inhibitors, which are the most potent known to date, show potential for the treatment of cancer in two ways: i) they exhibit cytotoxicity towards cancer derived cell lines and ii) they cause malignant cells to differentiate into non-cancerous cells.  The efficacy of these compounds is even more pronounced when used in combination with the known chemotherapeutic doxorubicin.  

 

Patent Information:
Title App Type Country Serial No. Patent No. File Date Issued Date Expire Date Patent Status
Protein Arginine Deiminase inhibitors as a novel therapeutic strategy for rheumatoid arthritis, cancer and other human diseases PCT United States PCT/US10/53944 10/25/2010      
Protein Arginine Deiminase inhibitors as a novel therapeutic strategy for rheumatoid arthritis, cancer and other human diseases Utility United States 13/503,446 8,921,595 10/25/2010 12/30/2014 8/16/2031  
For Information, Contact:
Technology Commercialization
University of South Carolina
technology@sc.edu
Inventors:
Paul Thompson
Corey Causey
Keywords:
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