【摘要】 大概1/3的人类癌症存在Ras原癌基因的突变,而Ras蛋白对于细胞的增殖分化等生理过程有着至关重要的作用,这使得Ras蛋白成为众人争相研究的对象。经过30多年的研究,发现Ras蛋白由于缺乏合适的药物分子结合口袋,难以成为有效的药物靶点蛋白,甚至认为"无药可成"。然而,近几年来结构生物学和生物信息学的不断发展,越来越多的证据表明Ras蛋白可以成为药物分子作用的靶点蛋白。本文综述了近几年来以Ras蛋白为靶点的抗癌药物研究进展,旨在为同类研究提供参考。更多还原

【Abstract】 Mutations in the Ras oncogene occur in about one-third of human cancers,and Ras proteins play a crucial role in many physiological processes,such as cell proliferation and differentiation,making Ras proteins a subject of intense researches. After more than 30 years of research,it is found that Ras proteins are difficult to develop as an effective drug target due to lacking of a suitable binding pocket,and even considered"undruggable". However,in recent years,with the development of structural biology and bioinformatics,there is increasing evidence proving that Ras proteins could be a kind of target protein for small molecules. In this paper,the research progress of anticancer agents targeting Ras proteins in recent years is reviewed aiming to provide corresponding references for similar researches.更多还原