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Peloruside A,一种具有类似紫杉醇微管稳定活性的新型抗有丝分裂剂。

Peloruside A, a novel antimitotic agent with paclitaxel-like microtubule- stabilizing activity.

作者信息

Hood Kylie A, West Lyndon M, Rouwé Berber, Northcote Peter T, Berridge Michael V, Wakefield St John, Miller John H

机构信息

School of Biological Sciences, Victoria University of Wellington, New Zealand.

出版信息

Cancer Res. 2002 Jun 15;62(12):3356-60.

Abstract

Peloruside A is a novel secondary metabolite isolated from a New Zealand marine sponge, Mycale hentscheli, that has potent paclitaxel-like microtubule-stabilizing activity and is cytotoxic at nanomolar concentrations. Its 16-membered macrolide ring is similar to that of epothilone, a drug currently under clinical investigation as an anticancer agent. Like paclitaxel, peloruside A arrests cells in the G(2)-M phase of the cell cycle and induces apoptosis. The relatively simple structure of peloruside makes it suitable for the design and synthesis of analogues with improved tumor targeting and reduced tumor cross-resistance.

摘要

Peloruside A是从新西兰海洋海绵Mycale hentscheli中分离出的一种新型次生代谢产物,具有类似紫杉醇的强大微管稳定活性,在纳摩尔浓度下具有细胞毒性。其16元大环内酯环与埃坡霉素相似,埃坡霉素是一种目前正在进行抗癌临床研究的药物。与紫杉醇一样,Peloruside A使细胞停滞在细胞周期的G(2)-M期并诱导细胞凋亡。Peloruside相对简单的结构使其适合设计和合成具有改善的肿瘤靶向性和降低的肿瘤交叉耐药性的类似物。

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