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• W2808068699 abstract "Since cells in solid tumors divide less rapidly than cells in the bone marrow or cells of the immune system, mitotic inhibitors often cause severe side effects when used for treatment of diseases like prostate cancer and breast cancer. One approach to overcome this problem involves attempts at developing drugs based on general cytotoxins, like calicheamicin and thapsigargin, which kill cells at all phases of the cell cycle. However, such toxins can only be used when efficient targeting to the malignant tissue is possible. In the case of thapsigargin, selectivity for tumor-associated cells is achieved by conjugating the drug to a peptide that is only cleaved in the vicinity of tumors to release the cytotoxic drug or an analog with retained activity. Solid-phase synthesis protocols were developed for preparation of three already validated prodrugs of thapsigargin: one prodrug cleavable by human kallikrein 2, one prodrug cleavable by prostate-specific antigen, and one prodrug cleavable by prostate-specific membrane antigen." @default.
• W2808068699 created "2018-06-21" @default.
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• W2808068699 date "2018-06-15" @default.
• W2808068699 modified "2023-09-26" @default.
• W2808068699 title "Preparation of Enzyme-Activated Thapsigargin Prodrugs by Solid-Phase Synthesis" @default.
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• W2808068699 doi "https://doi.org/10.3390/molecules23061463" @default.
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