摘要
背景:微管靶向药物(MTAs)是最成功的癌症化疗抗癌药物。MTAs通过干扰微管蛋白聚合和解聚动力学,影响细胞内转运和细胞信号通路,抑制细胞有丝分裂和细胞增殖,诱导细胞凋亡和死亡。微管蛋白maytansin位点结合剂是天然或天然衍生的产物,代表一种MTAs,可抑制微管蛋白聚合,并在体内外均表现出强大的抗肿瘤活性。它们在癌症化疗中被用作抗体-药物偶联物(ADCs)。 方法:以SciFinderR为工具,对有关maytansine及其衍生物、maytansine结合位点、maytansine位点结合剂及其作为MTAs在癌症治疗中的应用进行调查,排除作为专利发表的文献。临床试验的最新进展可从临床试验网站获得。 结果:本文介绍了MTAs、maytansin、maytansin结合位点及其配体,以及这些配体作为MTAs和ADCs在肿瘤治疗中的应用。 结论:maytansin位点结合剂是肿瘤化疗的强效MTAs。基于maytansin位点配体的ADCs被用于临床或临床试验中作为癌症靶向治疗,以提高其选择性并减少其副作用。进一步提高ADCs的传递效率将有利于肿瘤靶向治疗的患者。
关键词: 微管靶向药物,maytansin结合位点,根瘤毒素,普洛卡布林,抗体-药物偶联物,曲妥珠单抗。
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