[PDF][PDF] YAP/TAZ inhibition induces metabolic and signaling rewiring resulting in targetable vulnerabilities in NF2-deficient tumor cells

SM White, ML Avantaggiati, I Nemazanyy, C Di Poto… - Developmental cell, 2019 - cell.com
SM White, ML Avantaggiati, I Nemazanyy, C Di Poto, Y Yang, M Pende, GT Gibney…
Developmental cell, 2019cell.com
Merlin/NF2 is a bona fide tumor suppressor whose mutations underlie inherited tumor
syndrome neurofibromatosis type 2 (NF2), as well as various sporadic cancers including
kidney cancer. Multiple Merlin/NF2 effector pathways including the Hippo-YAP/TAZ pathway
have been identified. However, the molecular mechanisms underpinning the growth and
survival of NF2-mutant tumors remain poorly understood. Using an inducible orthotopic
kidney tumor model, we demonstrate that YAP/TAZ silencing is sufficient to induce …
Summary
Merlin/NF2 is a bona fide tumor suppressor whose mutations underlie inherited tumor syndrome neurofibromatosis type 2 (NF2), as well as various sporadic cancers including kidney cancer. Multiple Merlin/NF2 effector pathways including the Hippo-YAP/TAZ pathway have been identified. However, the molecular mechanisms underpinning the growth and survival of NF2-mutant tumors remain poorly understood. Using an inducible orthotopic kidney tumor model, we demonstrate that YAP/TAZ silencing is sufficient to induce regression of pre-established NF2-deficient tumors. Mechanistically, YAP/TAZ depletion diminishes glycolysis-dependent growth and increases mitochondrial respiration and reactive oxygen species (ROS) buildup, resulting in oxidative-stress-induced cell death when challenged by nutrient stress. Furthermore, we identify lysosome-mediated cAMP-PKA/EPAC-dependent activation of RAF-MEK-ERK signaling as a resistance mechanism to YAP/TAZ inhibition. Finally, unbiased analysis of TCGA primary kidney tumor transcriptomes confirms a positive correlation of a YAP/TAZ signature with glycolysis and inverse correlations with oxidative phosphorylation and lysosomal gene expression, supporting the clinical relevance of our findings.
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