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 Position: Home > issue > The 2nd Issue  
Overcoming resistance to drugs targeting KRASG12C mutation
Category: Review
Author: Shengyu Yang

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Overcoming resistance to drugs targeting KRASG12C mutation


Activating KRAS mutations are presented in 25% of human cancer. Although oncogenic Ras was deemed ¡®undruggable¡¯ in the past, recent efforts led to the development of pharmacological inhibitors targeting the KRASG12C mutant, which have shown promise in early clinical trials. The development of allele-specific K-RasG12C inhibitors marked a new chapter in targeting oncogenic KRAS mutant in cancer. However, drug resistance against these new drugs will likely limit their efficacy in the clinic. Genome-wide approaches have been used to interrogate the mechanisms of resistance to K-RasG12C inhibitors, which would facilitate the development of therapeutics overcoming drug resistance. This article reviews the latest progress in resistance to K-RasG12C-targeted therapies and aims to provide insight in future research targeting drug resistance in cancer.





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