Novel Non-ATP Competitive SRC Inhibitor for Treating Cancer

Description:

Project ID:  D2009-07

 

Background:P

SRC kinase inhibitors have been clinically tested on a number of cancers.  These inhibitors work by interrupting SRC’s role in tumor growth, proliferation, adhesion and motility.  The most common method of inhibiting SRC is through an ATP analog, blocking the ATP binding site.  However, ATP analogs have relatively low specificity since ATP is a common substrate.  ATP analogs must be administered in low concentration so that they do not interfere with non-targeted kinases.  In order to achieve a higher level of specificity, ATP analogs are designed to fit into a highly specific binding site.  However, the precise nature of this interaction means that any minor structural changes, such as through a single nucleotide mutation, could render the ATP analog ineffective.

Invention Description:

Invention describes novel non-ATP competitive SRC inhibitor for treating cancer.  Dr. Xie has identified a cell-permeable, 20 amino acid peptide that specifically disrupts SRC.  The peptide is capable of inducing cell death in human cancer cells, including prostate cancer cells, breast cancer cells, and neuroblastoma cells.  Administration of the peptide also significantly inhibits the growth of prostate cancer xenograft in mice. 

Advantages:

·       SRC is a well-established target in cancer treatment

·       Non-ATP analog SRC inhibitor provides much greater specificity

Applications:

·       Treatment of human cancers, such as prostate and breast cancer

·       Use of this non-ATP interaction site to develop a small molecule inhibitor specific to SRC

 

IP Status:  U.S. Utility patent pending

Patent Information:
For Information, Contact:
Stephen Snider
AVP Tech Transfer
The University of Toledo
419 530 6225
Stephen.Snider@utoledo.edu
Inventors:
Zi-Jian Xie
Zhichuan Li
Joseph Shapiro
Keywords:
Breast
Cancer
Neuroblastoma
Prostate
Src inhibitor