Synthesis and Use of Novel Inhibitors and Inactivators of Protein Arginine Deiminases

Description:

Reference #:  00593

The University of South Carolina is offering licensing opportunities for this technology.

Invention Description:

This invention is the design, synthesis, and in vitro evaluation of two fluorescently labeled activity-based protein profiling (ABPP) reagents that specifically and irreversibly modify the active form of PAD4 with great affinity.  

Background:

Protein arginine deiminase 4 (PAD4), which catalyzes the post-translational conversion of peptidyl arginine to peptidyl citrulline, is widely regarded as one of the best new targets for the development of a novel rheumatoid arthritis therapeutic. In addition to its presumed role in this disease, PAD4 is also a calcium-dependent histone deiminase that acts as a transcriptional co-repressor.

Potential Applications:

The fluorescently tagged ABPPs will be useful for identifying the conditions under which this enzyme is activated in vivo and may prove to be useful RA diagnostics.

Advantages and Benefits:

Specifically, these ABPPs will be useful for identifying the in vivo conditions under which this enzyme is activated; that is, they will help to determine if post-translational modifications, such as proteolytic processing, occur to this enzyme during its in vivo activation, potentially offering an explanation for why nonphysiological concentrations of calcium are required for in vitro enzyme activity. Furthermore, these probes may prove to be useful RA diagnostics and will undoubtedly aid the identification of nonspecific targets of these compounds whose identities will aid the successful design and synthesis of PAD4-specific inhibitors.

Patent Information:
Title App Type Country Serial No. Patent No. File Date Issued Date Expire Date Patent Status
Synthesis and Use of Novel Inhibitors and Inactivators of Protein Arginine Deiminases PCT United States PCT/US2006/043378 11/7/2006     Expired
Synthesis and Use of Novel Inhibitors and Inactivators of Protein Arginine Deiminases Nationalized PCT United States 12/092,627 7,964,636 9/19/2008 6/21/2011 11/7/2026 Issued
For Information, Contact:
Technology Commercialization
University of South Carolina
technology@sc.edu
Inventors:
Paul Thompson
Yuan Luo
Keywords:
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