TAXOL - MECHANISMS OF ACTION AND RESISTANCE
TAXOL - MECHANISMS OF ACTION AND RESISTANCE
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DOI：
10.1111/j.1749-6632.1986.tb38455.x
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发表时间：
1986-06-30
影响因子：
5.2
通讯作者：
ZEHEB, R
中科院分区：
文献类型：
--
作者：
HORWITZ, SB;LOTHSTEIN, L;ZEHEB, R
紫杉醇是在1971年从紫杉科成员短叶红豆杉的茎皮中分离出来的。它和相关的化合物也被发现在叶子，茎，和各种其他红豆杉物种的根。2在实验鼠系统中，紫杉醇已被证明具有抗白血病和肿瘤抑制特性，目前正在人体I期临床试验中进行测试。这种药物是一种复杂的酯，由具有氧杂环丁烷环的紫杉烷衍生物组成，氧杂环丁烷环是一种不寻常的化学结构，其生物活性以前没有研究过。紫杉醇已成为研究微管结构和功能的重要工具。它补充了其他植物生物碱，如秋水仙碱，鬼臼毒素和长春花生物碱，作为一种探针，用于阐明涉及微管的聚合和解聚的复杂机制。下面的讨论将回顾我们实验室对紫杉醇的作用机制和耐药性的研究。
Taxol was isolated in 1971 from the stem bark of the plant, Taxus brevifolia, a member of the yew family.'It and related compounds have also been found in the leaves, stems, and roots of a variety of other Taxus species. 2 In experimental murine systems, taxol has demonstrated antileukemic and tumor inhibitory properties and is presently being tested in Phase I clinical trials in humans. This drug is a complex ester consisting of a taxane derivative with an oxetan ring, an unusual chemical structure whose biological activity had not been previously studied. Taxol has become an important tool for studying the structure and function of microtubules. It complements other plant alkaloids such as colchicine, podophyllotoxin, and the vinca alkaloids, as a probe for elucidating the complex mechanisms involved in the polymerization and depolymerization of microtubules. The following discussion will review the research that has been done in our laboratory to study the mechanism of action and of resistance to taxol.