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Photodynamic therapy (PDT) is a treatment modality for destruction of tumor cells pathogenic microbes. This technology is based on the light excitation of a photosensitizer (PS) which induces oxidative damages at the cellular membrane or within the cells by formation of reactive oxygen species. However, the lack of selective accumulation of these molecules within tumor tissue or microbial cells is a major problem in PDT. Targeted PDT offers the opportunity of enhancing photodynamic efficiency by directly targeting diseased cells and tissues. Many attempts have been made to either increase the cellular uptake of the PSs by the target cells and tissues and/or to improve subcellular (e.g., mitochondria, nucleus) localization. The principal means to achieve targeting include passive delivery or the synthesis of bioconjugates with recognition unit (e.g., receptor ligand, monoclonal antibody) in which PS is covalently attached to biomolecules. This review outlines recent advances and the actual state of the developments including the synthesis and functional characterisation of porphyrinoid photosensitizers covalently conjugated with peptides or proteins.

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