Jordan A, Hadfield J A, Lawrence N J, McGown A T
Department of Chemistry, University of Manchester Institute of Science and Technology, UK.
Med Res Rev. 1998 Jul;18(4):259-96. doi: 10.1002/(sici)1098-1128(199807)18:4<259::aid-med3>3.0.co;2-u.
Tubulin is the biochemical target for several clinically used anticancer drugs, including paclitaxel and the vinca alkaloids vincristine and vinblastine. This review describes both the natural and synthetic agents which are known to interact with tubulin. Syntheses of the more complex agents are referenced and the potential clinical use of the compounds is discussed. This review describes the biochemistry of tubulin, microtubules, and the mitotic spindle. The agents are discussed in relation to the type of binding site on the protein with which they interact. These are the colchicine, vinca alkaloid, rhizoxin/maytansine, and tubulin sulfhydryl binding sites. Also included are the agents which either bind at other sites or unknown sites on tubulin. The literature is reviewed up to October 1997.
微管蛋白是几种临床使用的抗癌药物的生化靶点，包括紫杉醇以及长春花生物碱长春新碱和长春碱。本综述描述了已知与微管蛋白相互作用的天然和合成药物。文中引用了更复杂药物的合成方法，并讨论了这些化合物的潜在临床用途。本综述描述了微管蛋白、微管和有丝分裂纺锤体的生物化学。根据药物与蛋白质相互作用的结合位点类型对这些药物进行了讨论。这些位点包括秋水仙碱、长春花生物碱、根霉素/美登木素以及微管蛋白巯基结合位点。还包括那些在微管蛋白上其他位点或未知位点结合的药物。本文对截至1997年10月的文献进行了综述。
