An image contrast agent selectively activated by prostate specific antigen
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- 作者：Graham B. Jones ; Curtis F. Crasto ; Jude E. Mathews ; Longfei Xie ; Miguel O. Mitchell ; Ahmed El-Shafey ; Anthony V. D’ ; Amico and Glenn J. Bubley
- 关键词：Enzyme substrates ; PSA ; Linker ; Imaging agents ; Chemical synthesis ; Prodrugs ; Coumarin ; Hexapeptides
- 刊名：Bioorganic and Medicinal Chemistry
- 出版年：2006
- 出版时间：15 January 2006
- 年：2006
- 卷：14
- 期：2
- 页码：418-425
- 全文大小：166 K
文摘
A family of image contrast agent conjugates designed to undergo enzymatic activation has been synthesized. The agents underwent activation both with enzymatically active prostate specific antigen (PSA) and α-chymotrypsin, releasing free fluorophore via cleavage of a three-component system. A hexapeptide derivative showed exclusive activation by PSA and constitutes a method for tracking PSA activity in vitro.