Small molecules that reactivate mutant p53
Small molecules that reactivate mutant p53
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DOI：
10.1016/s0959-8049(03)00454-4
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发表时间：
2003-09-01
影响因子：
8.4
通讯作者：
Wiman, KG
中科院分区：
文献类型：
--
作者：
Bykov, VJN;Selivanova, G;Wiman, KG
大约一半的人类肿瘤携带突变型 p53。这使得可以逃避 p53 诱导的细胞周期停滞和细胞凋亡。许多肿瘤表达突变 p53 蛋白的水平升高。野生型p53功能的恢复应该会引发肿瘤细胞的大量凋亡，从而根除肿瘤。已鉴定出多种类型的小分子可以恢复突变 p53 的天然构象和野生型功能。这些分子可以作为开发新型有效抗癌药物的先导。 (C) 2003 年，爱思唯尔有限公司出版。
Around half of all human tumours carry mutant p53. This allows escape from p53-induced cell cycle arrest and apoptosis. Many tumours express mutant p53 proteins at elevated levels. Restoration of wild-type p53 function should trigger massive apoptosis in tumour cells and thus eradicate tumours. Various types of small molecules have been identified that can restore native conformation and wild-type function to mutant p53. Such molecules may serve as leads for the development of novel efficient anticancer drugs. (C) 2003 Published by Elsevier Ltd.