Article
Classical RAS proteins are not essential for paradoxical ERK activation induced by RAF inhibitors.
Proceedings of the National Academy of Sciences of the United States of America - 1 Feb 2022
Lai Lick Pui, Fer Nicole, Burgan William, Wall Vanessa E, Xu Bingfang, Soppet Daniel, Esposito Dominic, Nissley Dwight V, McCormick Frank
Abstract excerpt
RAF inhibitors unexpectedly induce ERK signaling in normal and tumor cells with elevated RAS activity. Paradoxical activation is believed to be RAS dependent. In this study, we showed that LY3009120, a pan-RAF inhibitor, can unexpectedly cause paradoxical ERK activation in KRASG12C-dependent lung cancer cell lines, when KRAS is inhibited by ARS1620, a KRASG12C inhibitor. Using H/N/KRAS-less mouse embryonic...
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