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Novel Non-ATP Competitive SRC Inhibitor for Treating Cancer

详细技术说明

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 specificityApplications:·       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

*Abstract

*Principal Investigation

Name: Zi-Jian Xie, Associate Professor

Department: Phys Pharm. Met/Cardio Science

Name: Zhichuan Li, Assistant Professor

Department: Medicine

Name: Joseph Shapiro, Dean

Department: Medicine

国家/地区

美国