The use of dipeptide derivatives of 5-aminolaevulinic acid promotes their entry to tumor cells and improves tumor selectivity of photodynamic therapy
- Di Venosa, Gabriela Mariana
- Vallecorsa, Pablo Daniel
- Giuntini, Francesca
- Mamone, Leandro Ariel
- Batlle, Alcira María del C.
- Vanzuli, Silvia
- Juarranz, Ángeles
- MacRobert, Alexander J.
- Egglestone, Ian M.
- Casas, Adriana Gabriela
DOIAbstract
The use of endogenous protoporphyrin IX generated after administration of 5-aminolaevulinic acid (ALA) has led to many applications in photodynamic therapy (PDT). However, the bioavailability of ALA is limited by its hydrophilic properties and limited cell uptake. A promising approach to optimize the efficacy of ALA-PDT is to deliver ALA in the form of prodrugs to mask its hydrophilic nature. The aim of this work was to evaluate the potential of two ALA dipeptide derivatives, N-acetyl terminated leucinyl-ALA methyl ester (Ac-Leu-ALA-Me) and phenylalanyl-ALA methyl ester (Ac-Phe-ALA-Me), for their use in PDT of cancer, by investigating the generation of protoporphyrin IX in an oncogenic cell line (PAM212-Ras), and in a subcutaneous tumor mod...
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