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首页> 外文期刊>Drug discovery today >Therapeutic modulation of k-ras signaling in colorectal cancer.
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Therapeutic modulation of k-ras signaling in colorectal cancer.

机译:大肠癌中k-ras信号的治疗性调节。

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摘要

KRAS has an important role in colorectal carcinogenesis and mutant KRAS leads to a permanently activated k-ras protein. To exert its biological activity, k-ras requires post-translational modification by prenylation. K-ras modulation has become a promising concept for new therapies, mostly by interference with the mevalonate pathway and subsequently by the prenylation of k-ras. Clinical data of agents interfering with the mevalonate pathway and the prenylation of ras are summarized and suggest that these agents might be effective when administered in combination with anticancer drugs that target k-ras. Here, we discuss the novel concept that modulation of k-ras might potentiate EGFR therapy by altering the KRAS phenotype.
机译:KRAS在结直肠癌发生中起重要作用,而突变KRAS导致永久激活的k-ras蛋白。为了发挥其生物学活性,k-ras需要通过异戊二烯化作用进行翻译后修饰。 K-ras调制已成为新疗法的一个有前途的概念,主要是通过干扰甲羟戊酸途径并随后通过k-ras的异戊二烯化来实现的。总结了干扰甲羟戊酸途径和ras异戊二烯的药物的临床数据,并表明这些药物与靶向k-ras的抗癌药物联合给药可能有效。在这里,我们讨论了新的概念,即调节k-ras可能通过改变KRAS表型来增强EGFR治疗。

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