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Cyclopeptidic-based protease-sensitive photosensitizer prodrugs for selective photodynamic therapy

Univ Genève. 2018; 
Bouilloux, Jordan
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Biochemicals Formic acid (FA, 98-100%) was purchased from Merck (Darmstadt, Germany). O-(7-azabenzotriazole-1-yl)- N,N,N’N’-tetramethyluronium hexafluorophosphate (HATU) was obtained from GenScript Corporation (Piscataway, New Jersey, USA). Get A Quote

摘要

In photodynamic therapy (PDT), high polydispersity of polymeric carriers and random distribution of loaded photosensitizers (PSs) result in batch-to-batch variabilities. Alternatively, we designed cyclopeptidic photosensitizer prodrugs (cPPPs). These conjugates are perfectly defined, non-toxic and optically extinct in their initial state, reducing the side effects of premature exposure to radiation. Thanks to copper-free click chemistry, we coupled various loading of PSs, quenchers and chemotherapeutic drugs onto constrained scaffolds through protease-sensitive peptidic linkers. In the context of PDT use, relevant cPPPs are activated in vitro by enzymes (e.g., urokinase, cathepsin B) overexpressed by cancer cel... More

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