Carbohydrate Dependent Targeting Of Cancer Cells By Bleomycin-microbubble Conjugates

摘要

The bleomycins (BLM A_5,1) are clinically used antitumor agents efficacious in the treatment of squamous cell carcinomas and malignant lymphomas. Their antitumor activity is believed to result from their ability to mediate the selective oxidative cleavage of DNA and possibly also RNA.rnOne property of bleomycin that has been recognized for decades is its ability to target tumors; this has been documented in numerous tumor imaging studies that employed BLMs bound to radionuclides. The importance of tumor targeting to the therapeutic efficacy of BLM is underscored by the therapeutic dose of BLM (～5 μmol), which is quite low relative to the doses of many clinically used agents. Understanding the molecular nature of tumor targeting by BLM would facilitate the synthesis of analogues with improved properties and might also enable the selective delivery of other probes and drugs to tumor cells.