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AbstractA Swiss academic research lab has developed novel highly specific photosensitizer prodrugs (PPs).These PPs only release cytotoxic reactive oxygen species when activated by the unique combination of disease-associated proteolytic activity and light. As a result, any type of cell overexpressing a chosen protease can be targeted for destruction. Targeted diseases include cancer, rheumatoid arthritis and bacterial infection. Industrial partners are sought for in-licensing or technical collaboration.DetailsRemoving diseased cells without damaging neighboring tissue is a major challenge in the treatment of cancer, rheumatoid arthritis or bacterial infections. Photodynamic therapy (PDT) is a selective treatment modality based on the accumulation of a photosensitive agent in the target tissue. The very short action range of reactive oxygen species (ROS), produced upon excitation of the photosensitive agent with light, leads to cell death only in areas where the agent has accumulated.The limited selectivity of conventional photosensitizer drugs can lead collateral damage to vital structures in the direct environment of the irradiation site and whole-body photosensitization, where patients need to avoid exposure to sunlight for weeks to avoid severe skin and eye damage. To avoid these drawbacks related to poor selectivity and ensure that only diseased cells are targets of PDT, the laboratory has developed highly specific photosensitizer prodrugs (PPs) tailored to disease-associated proteolytic activity. These PPs only generate cytotoxic reactive oxygen species (ROS) when activated by the unique combination of a specific protease and exposure to light. Innovative Aspects: - Highly selective for chosen protease, sparing neighboring tissue, - Fully customizable, from protease to wavelength of light source, - Water-soluble, even with highly lipophilic photosensitizers, - Easy to synthesize, with high yields and high purity, - Synthetic strategy can be adapted to any photosensitizers.
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