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Taccalonolides: a microtubule stabilizer poses a new puzzle with old pieces.

机译:Taccalonolides:微管稳定剂带来了旧碎片的新难题。

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The structural diversity of microtubule targeting agents (MTAs) is breathtaking, from simple bicyclics, like combretastatins, to complex compounds, like epothilones and halicondrins. The taccalonolides, plant-derived steroids described by Risinger and Mooberry in the July 1st issue of Cell Cycle, fall somewhere in the middle of this structural complexity.Interest in MTAs as chemotherapeutics began with the use of vincristine to treat acute lymphoblastic leukemia in the 1950s and shows no sign of abating. All MTAs inhibit mitosis in rapidly growing cells, though clinical efficacy against patient tumors is likely due to non-mitotic activities. The success of MTAs as chemotherapeutics has fueled searches for new compounds, one result being the taccalonolides.
机译:微管靶向剂(MTA)的结构多样性令人叹为观止,从简单的双环化合物(如康培他汀)到复杂的化合物(如埃坡霉素和halicondrins)。 Raccinger和Mooberry在7月1日的《细胞周期》(Cell Cycle)一书中描述的植物源性类固醇类化合物taccalonolides处于这种结构复杂性的中间位置.1950年代开始使用长春新碱治疗急性淋巴细胞白血病时,化学疗法开始对MTA产生兴趣。并没有减弱的迹象。所有的MTA都抑制快速生长的细胞中的有丝分裂,尽管针对患者肿瘤的临床疗效可能是由于非有丝分裂活动所致。 MTA作为化学治疗剂的成功推动了对新化合物的搜寻,其中一个结果就是他卡洛酮。

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