Abstract：
:A new approach to selective photodynamic therapy (PDT) was developed by designing chlorin e6 (Ce6)-containing macromolecules, which are sensitive to tumor-associated proteases. The agents are nontoxic in their native state but become fluorescent and produce singlet oxygen on protease conversion. Coupled with optimized delivery systems, we show that (a) the agents efficiently accumulate in tumors due to the enhanced permeability and retention effect, (b) the agents are locally activated by proteases, (c) local drug concentrations can be measured by quantitative fluorescence tomography, and (d) light-treated tumors show reduced growth. A single low dose of PDT (0.125 mg Ce6 equivalent/kg) was sufficient to suppress tumor growth by >50%. Activatable singlet oxygen generation agents provide increased efficacy with reduced toxicity, and it could become a powerful PDT.
journal_name
Cancer Resjournal_title
Cancer researchauthors
Choi Y,Weissleder R,Tung CHdoi
10.1158/0008-5472.CAN-06-0448subject
Has Abstractpub_date
2006-07-15 00:00:00pages
7225-9issue
14eissn
0008-5472issn
1538-7445pii
66/14/7225journal_volume
66pub_type
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