Synthesis and Characterization of the Novel Stromelysine-1 and Prostate- Specific Antigen (PSA) Probes for Optical Imaging

• Main Authors: Wei-Hsan Chao, 趙尉善
• Other Authors: Yun-Ming Wang
• Format: Others
• Language: zh-TW
• Published: 2004
• Online Access: http://ndltd.ncl.edu.tw/handle/95655250461765237718

碩士 === 高雄醫學大學 === 醫藥暨應用化學系碩士班 === 92 === Near-infrared (NIR) fluorescence light has been applied to image various biological events in vivo, because it penetrates tissue more efficiently than light in the visible spectrum. Two 11 amino acids peptide substrates were designed and synthesized for specific enzyme Matrix Metalloproteinase-3 (MMP-3) and prostate-specific antigen (PSA) which are known to be overexpressed in antiarthritic and prostate cancer, respectively. A NIR cyanine fluorochrome served as the optical can be used for in vivo imaging of enzyme activity and is attached to the amino terminal of peptide substrate with specificity for MMP-3 and PSA. The PGC consisting of a poly-L-lysine (PL) backbone and methoxy poly(ethylene glycol) (MPEG) side chains was prepared. Peptide substrate was subsequently attached to a synthesis graft copolymer and another binding to fluorochrome Cy5.5. The ability of MMP-3 and PSA to recognize the peptide substrates was initially confirmed by HPLC. The HPLC elution chromatography was showed that one major cut of the stromelysine-1 and prostate peptide substrate in the presence of MMP-3 and prostate two fragments. Upon proteinase cleavage, the NIR probes fluorescence can be detected by fluorescence spectrophometer.