微管蛋白和微管作为抗癌药物的靶点。

Tubulin and microtubules as targets for anticancer drugs.

作者信息

Hadfield John A, Ducki Sylvie, Hirst Nicholas, McGown Alan T

机构信息

Centre for Molecular Drug Design, Department of Chemistry, University of Salford, Manchester, M5 4WT, UK.

出版信息

Prog Cell Cycle Res. 2003;5:309-25.

PMID:14593726

Abstract

Microtubules are intracellular organelles formed from the protein tubulin. These organelles have a number of essential cellular functions including chromosome segregation, the maintenance of cell shape, transport, motility, and organelle distribution. Drugs that affect the tubulin-microtubule equilibrium (taxol, vinca alkaloids) are effective anticancer drugs. This review describes the molecular target, methods used in screening, the structures of compounds known to interact with tubulin, and the clinical use of these agents. In addition the ability of these agents to destroy tumour vasculature is described. This represents an exciting new molecular target in the design of anticancer drugs.

摘要

微管是由微管蛋白形成的细胞内细胞器。这些细胞器具有许多重要的细胞功能，包括染色体分离、细胞形状维持、运输、运动及细胞器分布。影响微管蛋白-微管平衡的药物（紫杉醇、长春花生物碱）是有效的抗癌药物。本综述描述了分子靶点、筛选所用方法、已知与微管蛋白相互作用的化合物结构以及这些药物的临床应用。此外，还描述了这些药物破坏肿瘤脉管系统的能力。这代表了抗癌药物设计中一个令人兴奋的新分子靶点。