【摘要】 海兔毒素10(dolastatin 10,D10)是从海洋无壳软体动物截尾海兔(Dolabella auricularia)中分离提取的由4个氨基酸组成的线性缩肽类天然毒性蛋白。dolastatin 10及其衍生物可以抑制细胞有丝分裂,具有很强的抗肿瘤活性,已进入临床研究阶段。文中综述对dolastatin 10的发现、结构特点与作用机制,其衍生物及衍生物与相应单克隆抗体偶联物的临床疗效。更多还原

【Abstract】 ] Dolastatin 10,a cytostatic depsipeptide containing four unique amino acid subunits,was isolated from the marine shell-less mollusk Dolabella auricularia.Dolastatin 10 and its derivatives,which demonstrated antimitotic,antiproliferative and growth inhibitary activities in tumor cells through inhibition of tubulin polymerization,have been used in clinical studies.In this review,we described the discovery,cytotoxicity,structure features,action mechanism and clinical studies of dolastatin 10.The therapeutic efficacy of dolastatin 10 derivatives and their monoclonal antibody conjugates were particularly discussed.更多还原