STUDIES WITH RP-56976 (TAXOTERE) - A SEMISYNTHETIC ANALOG OF TAXOL
STUDIES WITH RP-56976 (TAXOTERE) - A SEMISYNTHETIC ANALOG OF TAXOL
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DOI：
10.1093/jnci/83.4.288
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发表时间：
1991-02-20
期刊：
影响因子：
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通讯作者：
HORWITZ, SB
中科院分区：
文献类型：
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作者：
RINGEL, I;HORWITZ, SB
RP 56976（taxotere）是一种新的半合成紫杉醇类似物，是一种潜在的重要的抗癌化疗药物。 我们在这里报告说，这种药物是一种有效的细胞复制抑制剂，像紫杉醇，促进稳定的微管在体外组装的情况下，三磷酸鸟苷和诱导微管束形成细胞。 与紫杉醇相比，RP 56976作为微管蛋白聚合促进剂的活性略高。 作为细胞复制抑制剂，RP 56976在J774.2和P388细胞中的效力是紫杉醇的2.5倍，在紫杉醇耐药细胞中的效力至少是紫杉醇的5倍。
RP 56976 (taxotere), a new semisynthetic analogue of taxol, is a potentially important chemotherapeutic agent for the treatment of cancer. We report here that this drug is a potent inhibitor of cell replication and, like taxol, promotes the in vitro assembly of stable microtubules in the absence of guanosine triphosphate and induces microtubule-bundle formation in cells. Compared with taxol, RP 56976 is slightly more active as a promoter of tubulin polymerization. As an inhibitor of cell replication, RP 56976 is 2.5-fold more potent than taxol in J774.2 and P388 cells and at least 5-fold more potent in taxol-resistant cells.