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Becatecarin is a synthetic diethylaminoethyl (DEAE) analogue of the indolocarbazole glycoside antineoplastic antibiotic rebeccamycin. It is a water-soluble small molecule developed as an anticancer agent, primarily for the treatment of hepatobiliary duct tumors and biliary cancer, which are rare and aggressive cancers with limited treatment options. Becatecarin acts by intercalating into DNA and stabilizing the DNA-topoisomerase I complex, thereby interfering with topoisomerase I-catalyzed DNA breakage-reunion reactions. This leads to DNA cleavage and apoptosis in cancer cells. Becatecarin also exhibits activity as a weak substrate for the ABCG2 transporter, which may contribute to drug resistance in some tumor types[1][2][3][4][5].
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