DNA topoisomerase I--targeted chemotherapy of human colon cancer in xenografts
作者： B. Giovanella , J. Stehlin , M. Wall , M. Wani , A. Nicholas
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摘要: Drug development is needed to improve chemotherapy of patients with locally advanced or metastatic colon carcinoma, who otherwise have an unfavorable prognosis. DNA topoisomerase I, a nuclear enzyme important for solving topological problems arising during replication and other cellular functions, has been identified as principal target plant alkaloid 20(S)-camptothecin. Significantly increased concentrations this enzyme, compared that in normal colonic mucosa, were found stages human adenocarcinoma xenografts cancer carried by immunodeficient mice. Several synthetic analogs camptothecin, selected tests the purified tissue-culture screens, evaluated xenograft model. Unlike anticancer drugs tested, 20(RS)-9-amino-camptothecin (9-AC) induced disease-free remissions. The overall drug toxicity was low allowed repeated courses treatment.
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