SHOC2 phosphatase-dependent RAF dimerization mediates resistance to MEK inhibition in RAS-mutant cancers
GG Jones, IB Del Río, S Sari, A Sekerim… - Nature …, 2019 - nature.com
GG Jones, IB Del Río, S Sari, A Sekerim, LC Young, N Hartig, I Areso Zubiaur…
Nature communications, 2019•nature.comTargeted inhibition of the ERK-MAPK pathway, upregulated in a majority of human cancers,
has been hindered in the clinic by drug resistance and toxicity. The MRAS-SHOC2-PP1
(SHOC2 phosphatase) complex plays a key role in RAF-ERK pathway activation by
dephosphorylating a critical inhibitory site on RAF kinases. Here we show that genetic
inhibition of SHOC2 suppresses tumorigenic growth in a subset of KRAS-mutant NSCLC cell
lines and prominently inhibits tumour development in autochthonous murine KRAS-driven …
has been hindered in the clinic by drug resistance and toxicity. The MRAS-SHOC2-PP1
(SHOC2 phosphatase) complex plays a key role in RAF-ERK pathway activation by
dephosphorylating a critical inhibitory site on RAF kinases. Here we show that genetic
inhibition of SHOC2 suppresses tumorigenic growth in a subset of KRAS-mutant NSCLC cell
lines and prominently inhibits tumour development in autochthonous murine KRAS-driven …
Abstract
Targeted inhibition of the ERK-MAPK pathway, upregulated in a majority of human cancers, has been hindered in the clinic by drug resistance and toxicity. The MRAS-SHOC2-PP1 (SHOC2 phosphatase) complex plays a key role in RAF-ERK pathway activation by dephosphorylating a critical inhibitory site on RAF kinases. Here we show that genetic inhibition of SHOC2 suppresses tumorigenic growth in a subset of KRAS-mutant NSCLC cell lines and prominently inhibits tumour development in autochthonous murine KRAS-driven lung cancer models. On the other hand, systemic SHOC2 ablation in adult mice is relatively well tolerated. Furthermore, we show that SHOC2 deletion selectively sensitizes KRAS- and EGFR-mutant NSCLC cells to MEK inhibitors. Mechanistically, SHOC2 deletion prevents MEKi-induced RAF dimerization, leading to more potent and durable ERK pathway suppression that promotes BIM-dependent apoptosis. These results present a rationale for the generation of SHOC2 phosphatase targeted therapies, both as a monotherapy and to widen the therapeutic index of MEK inhibitors.
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