Journal
DYES AND PIGMENTS
Volume 195, Issue -, Pages -Publisher
ELSEVIER SCI LTD
DOI: 10.1016/j.dyepig.2021.109735
Keywords
Cancer; Photodynamic therapy; Leucine aminopeptidase; Hemicyanine; Activity-based photosensitizers
Funding
- BAGEP Award of the Science Academy
- Koc University
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Activity based photosensitizers are gaining attention for their selective action on cancer cells under light irradiation. A novel activatable PDT agent HCL was reported, selectively activated by the LAP enzyme in cancer cells with high LAP levels, showing effective photocytotoxicity with minimal dark toxicity. HCL could serve as an effective and tumor-associated LAP-sensitive phototheranostic agent.
Activity based photosensitizers (PS) continue to attract great attention as they enable selective photodynamic therapy action on cancer cells while sparing normal cells even under light irradiation. Sensitivity to specific enzymes that are differentially overexpressed in cancer cells is crucial in the design of activatable PSs. In this direction, we report here, for the first time, a leucine aminopeptidase (LAP) activatable PDT agent (HCL), which is a red-shifted, water soluble and photostable brominated hemicyanine derivative. HCL was activated by endogenous LAP enzyme selectively in A549 (lung) and HCT116 (colon) cancer cells containing high LAP levels and induced effective photocytotoxicity with negligible dark toxicity. Furthermore, the fluorescence of the parent bromo-hemicyanine core was restored upon LAP-based activation in cancer cells. On the other side, no remarkable phototoxicity or fluorescence turn-on was detected in healthy L929 cells. Thus, HCL serves as an effective and tumour associated LAP-sensitive phototheranostic agent. We believe different cancer-associated analytes can be utilized in combination with near-IR absorbing scaffolds in the scope of activatable PDT designs to enrich the tumour-selective PS arsenal.
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