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Studies with RP 56976 (taxotere): a semisynthetic analogue of taxol.

作者信息

Ringel I, Horwitz S B

机构信息

Department of Pharmacology, Hadassah Medical School, Hebrew University, Jerusalem, Israel.

出版信息

J Natl Cancer Inst. 1991 Feb 20;83(4):288-91. doi: 10.1093/jnci/83.4.288.

DOI:10.1093/jnci/83.4.288
PMID:1671606
Abstract

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.

摘要

相似文献

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Studies with RP 56976 (taxotere): a semisynthetic analogue of taxol.
J Natl Cancer Inst. 1991 Feb 20;83(4):288-91. doi: 10.1093/jnci/83.4.288.
2
Effects of Taxotere on murine and human tumor cell lines.多西他赛对小鼠和人类肿瘤细胞系的影响。
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Assembly of purified GDP-tubulin into microtubules induced by taxol and taxotere: reversibility, ligand stoichiometry, and competition.紫杉醇和多西他赛诱导纯化的GDP-微管蛋白组装成微管:可逆性、配体化学计量和竞争
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4
Solution structure of Taxotere-induced microtubules to 3-nm resolution. The change in protofilament number is linked to the binding of the taxol side chain.多西他赛诱导的微管的溶液结构解析至3纳米分辨率。原纤维数量的变化与紫杉醇侧链的结合有关。
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'Rings' of F-actin form around the nucleus in cultured human MCF7 adenocarcinoma cells upon exposure to both taxol and taxotere.在培养的人MCF7腺癌细胞中,暴露于紫杉醇和多西他赛后,F-肌动蛋白“环”会在细胞核周围形成。
Comp Biochem Physiol C Toxicol Pharmacol. 2000 Jan;125(1):121-31. doi: 10.1016/s0742-8413(99)00101-2.
6
Effects of Taxotere and taxol on in vitro colony formation of freshly explanted human tumor cells.泰索帝和紫杉醇对新鲜分离的人肿瘤细胞体外集落形成的影响。
Anticancer Drugs. 1992 Apr;3(2):121-4. doi: 10.1097/00001813-199204000-00008.
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Baccatin III induces assembly of purified tubulin into long microtubules.浆果赤霉素III诱导纯化的微管蛋白组装成长微管。
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Cancer Res. 1988 Jul 15;48(14):4093-100.
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Biologically active taxol analogues with deleted A-ring side chain substituents and variable C-2' configurations.具有缺失A环侧链取代基和可变C-2'构型的生物活性紫杉醇类似物。
J Med Chem. 1991 Mar;34(3):1176-84. doi: 10.1021/jm00107a042.
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Biochem Biophys Res Commun. 1984 Oct 30;124(2):329-36. doi: 10.1016/0006-291x(84)91557-2.

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