KRAS抑制剂的研究进展

Research progress of KRAS inhibitors

RAS(rat sarcoma)基因是一种重要的致癌基因,其突变存在于约30%的人类肿瘤中。KRAS(kirsten rat sarcoma viral oncogene)是RAS的三个亚型之一,且相比于其他两种RAS亚型更易出现突变。近年来,研究的不断深入为靶向KRAS治疗肿瘤提供了新的可能性,KRAS抑制剂的研发也因此取得了显著的进展。本文根据各类抑制剂的作用模式,将KRAS抑制剂分为直接靶向于KRAS的抑制剂和间接作用于KRAS的抑制剂两类,并由此综述介绍了具有代表性的KRAS抑制剂。

The RAS(rat sarcoma)gene is one of the important oncogenes,and its mutation is present in about30%human tumors.KRAS(kirsten rat sarcoma viral oncogene)is one of the three RAS subtypes,and KRAS mutations are more common than the mutations in other two RAS subtypes.In recent years,with the continuous research,new ideas have been provided for the treatment of cancers via targeting-KRAS.Efforts have been made to develop various KRAS inhibitors.Here,based on the mechanism of action,we classified KRAS inhibitors into two categories:inhibitors that directly target KRAS and inhibitors that indirectly act on KRAS.The representative KRAS inhibitors were summarized and introduced in this paper.