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• W2396533937 abstract "Photodynamic therapy (PDT) is based on the cytotoxicity of photosensitizers in the presence of light. Increased selectivity and effectivity of the treatment is expected if a specific uptake of the photosensitizers into the target cells, often tumor cells, can be achieved. An attractive transporter for that purpose is the folic acid receptor α (FRα), which is overexpressed on the surface of many tumor cells and mediates an endocytotic uptake. Here, we describe the synthesis and photobiological characterization of polar β-carboline derivatives as photosensitizers covalently linked to folate-tagged albumin as the carrier system. The particles were taken up by KB (human carcinoma) cells within <90 min and then co-localized with a lysosomal marker. FRα antibodies prevented the uptake and also the corresponding conjugate without folate was not taken up. Accordingly, a folate-albumin-β-carbolinium conjugate proved to be phototoxic, while the corresponding albumin-β-carbolinium conjugates without FA were nontoxic, both with and without irradiation. An excess of free folate as competitor for the FRα-mediated uptake completely inhibited the photocytotoxicity. Interestingly, the albumin conjugates are devoid of photodynamic activity under cell-free conditions, as shown for DNA as a target. Thus, phototoxicity requires cellular uptake and lysosomal degradation of the conjugates. In conclusion, albumin-folate conjugates appear to be promising vehicles for a tumor cell targeted PDT." @default.
• W2396533937 created "2016-06-24" @default.
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• W2396533937 date "2016-07-01" @default.
• W2396533937 modified "2023-10-18" @default.
• W2396533937 title "Albumin-Folate Conjugates for Drug-targeting in Photodynamic Therapy" @default.
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• W2396533937 doi "https://doi.org/10.1111/php.12602" @default.
• W2396533937 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/27221054" @default.
• W2396533937 hasPublicationYear "2016" @default.
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