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Article

Small-Molecule Inhibitors Directly Targeting KRAS as Anticancer Therapeutics.

Journal of medicinal chemistry - 10 Dec 2020

Chen Hao, Smaill Jeff B, Liu Tongzheng, Ding Ke, Lu Xiaoyun

Abstract excerpt

KRAS, the most frequently mutated oncogene, plays a predominant role in driving initiation and progression of cancers. Decades of effort to target KRAS using small molecules has been unsuccessful, causing KRAS to be considered an "undruggable" cancer target. However, this view began to change recently, as drug discovery techniques have developed several KRAS G12C allosteric inhibitors that are currently being...

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PMID: 33225706
DOI: 10.1021/acs.jmedchem.0c01312

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