Design and Synthesis of Renal Dipeptidase Inhibitors

Colon cancer is a deadly disease with a 6% average lifetime risk in the United States. When detected in the earliest stages, patients have a 90% survival rate. In the early stages of colon cancer, however, patients are generally asymptomatic. Therefore, colon cancer is often diagnosed in the late stages when there is only a 35% 5-year survival rate despite aggressive treatments. Previously, scientists from Johns Hopkins reported the use of serial analysis of gene expression (SAGE) to identify transcripts encoding secreted or cell surface proteins that were expressed in benign and malignant colorectal tumors. Several genes (TGFBI, LYS, RDP, MIC-1, REGA, and DEHL) were expressed at markedly higher levels in both benign and malignant tumors compared with normal colonic epithelium. One interesting gene identified in this study was renal dipeptidase (RDP). RDP is unique among the dipeptidases in that it can cleave amide bonds in which the COOH-terminal partner is a D-amino acid, providing an excellent opportunity for the development of specific probes for its detection in vivo. The present invention relates to novel RDP inhibitors which contain substituted aromatic side chain with radio labeled tag that can be used as biomarkers for detecting colon cancer at earlier stages. Description (Set) Proposed Use (Set) Specific chemical compounds designed and synthesized by Johns Hopkins scientists may be useful as biomarkers in detecting colon cancer in its early stages. Patent (Set) 6,927,212; WO 2004/10846

Inventor(s): Khan, Saeed R.

Type of Offer: Licensing



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