Prostate Activated Prodrugs and Imaging Agents
Abstract
The goal of this project is to demonstrate that enzymatically active prostate specific antigen (PSA) in the prostatic microenvironment can be used to locally activate either prodrugs or imaging systems. The substrate chosen was a 3 component system composed of a peptide sequence with affinity for PSA, an imaging agent and a deactivating bridge-linker, which electronically incapacitates the imaging agent. On PSA mediated release, the peptide sequence is designed to uncouple from the bridge, which then undergoes spontaneous decomposition, releasing free imaging agent The linker selected was 4-amino benzyl alcohol and proof of principle studies were conducted with a tyrosine derivative to which was coupled a series of 3 image contrast agents. The compounds underwent studies to evaluate enzymatic release on exposure to PSA, which successfully confirmed the design hypothesis.
Document Details
- Document Type
- Technical Report
- Publication Date
- May 01, 2004
- Accession Number
- ADA442972
Entities
People
- Graham B. Jones
Organizations
- Northeastern University