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レベッカマイシン(rebeccamycin)は、スタウロスポリンと構造的に類似している、Streptomyces sp.から単離された弱いトポイソメラーゼI阻害剤である。プロテインキナーゼあるいはトポイソメラーゼIIに対する阻害活性はほとんど示さない。In vitroで顕著な抗腫瘍作用を示す(IC50: 480 nM, マウスB16メラノーマ細胞、500 nM, P388白血病細胞)。 Lechevalieria aerocolonigenesから単離され、1985年に報告された。
, Rebeccamycin (NSC 655649) is a weak topois … Rebeccamycin (NSC 655649) is a weak topoisomerase I inhibitor isolated from Nocardia sp. It is structurally similar to staurosporine, but does not show any inhibitory activity against protein kinases. It shows significant antitumor properties in vitro (IC50=480nM against mouse B16 melanoma cells and IC50=500nM against P388 leukemia cells). It is an antineoplastic antibiotic and an intercalating agent. Becatecarin (BMS-181176) is a synthetic analog of rebeccamycin. Rebeccamycin and becatecarin have been tested in phase II clinical trials for the treatment of lung cancer, liver cancer, breast cancer, lymphoma, retinoblastoma, kidney cancer, and ovarian cancer.astoma, kidney cancer, and ovarian cancer.
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rdfs:comment |
レベッカマイシン(rebeccamycin)は、スタウロスポリンと構造的に類似している、Streptomyces sp.から単離された弱いトポイソメラーゼI阻害剤である。プロテインキナーゼあるいはトポイソメラーゼIIに対する阻害活性はほとんど示さない。In vitroで顕著な抗腫瘍作用を示す(IC50: 480 nM, マウスB16メラノーマ細胞、500 nM, P388白血病細胞)。 Lechevalieria aerocolonigenesから単離され、1985年に報告された。
, Rebeccamycin (NSC 655649) is a weak topois … Rebeccamycin (NSC 655649) is a weak topoisomerase I inhibitor isolated from Nocardia sp. It is structurally similar to staurosporine, but does not show any inhibitory activity against protein kinases. It shows significant antitumor properties in vitro (IC50=480nM against mouse B16 melanoma cells and IC50=500nM against P388 leukemia cells). It is an antineoplastic antibiotic and an intercalating agent. Becatecarin (BMS-181176) is a synthetic analog of rebeccamycin.76) is a synthetic analog of rebeccamycin.
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rdfs:label |
レベッカマイシン
, Rebeccamycin
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