For decades, mutant Ras (mut-Ras) proteins have been identified as drivers of multiple
cancers including pancreatic, lung, and colon cancers. However, targeting this oncogene has been
challenging and no Ras inhibitors are on the market to date. Lately several candidates targeting the
downstream pathways of Ras signaling, including PI3K and Raf, were approved for cancer treatment.
However, they do not present promising therapeutic effects on patients harboring Ras mutations.
Recently, a variety of compounds have been reported to impair the activity of Ras, and these exciting
discoveries reignite the hope for development of novel drugs targeting mut-Ras. In this article, we will
review the progress made in this field and the current state-of-the-art technologies to develop Ras inhibitors. Also we will
discuss the future direction of targeting Ras.
Keywords: Cancer therapy, Drug discovery, GTPase, Mutant KRas, Small molecule inhibitor, Targeting Ras.
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