Chloroacetamidine-based Inhibitors and Activity-based Probes for the Protein Arginine Methyltransferases


Reference #: 00771

Invention Description:

The present invention is a potent, irreversible inhibitor, targeting protein arginine methyltransferase 1. Inhibition studies have demonstrated that the inhibitor is a potent and selective inactivator of the enzyme. This inhibitor covalently modifies an active site residue on the enzyme.

Potential Applications:

This inhibitor could be a vital tool in the treatment of heart and vascular diseases. By regulating the levels of ADMA, NO synthesis can be increased, leading to improved vascular homeostasis. It is also believed that this inhibitor, or a derivative, can be useful in the treatment of breast cancer by helping to control PRMT1, debilitating early developing breast cancer cells.

Advantages and Benefits:

This inhibitor has a potency and selectivity ideal for generating therapeutic agents for the treatment of heart disease and breast cancer.

Patent Information:
Title App Type Country Serial No. Patent No. File Date Issued Date Expire Date Patent Status
Chloroacetamidine based inhibitors and activity based probes for the Protein Arginine Methyltransferases Utility United States 12/637,223 8,323,918 12/14/2009 12/4/2012 9/23/2030  
For Information, Contact:
Technology Commercialization
University of South Carolina
Paul Thompson
Tanesha Osborne
Obiamaka Obianyo
Corey Causey
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