Inhibition of mTORC1/2 overcomes resistance to MAPK pathway inhibitors mediated by PGC1α and Oxidative Phosphorylation in melanoma.
By: Y N Vashisht Gopal, Helen Rizos, Guo Chen, Wanleng Deng, Dennie T Frederick, Zachary A Cooper, Richard A Scolyer, Gulietta M Pupo, Kakajan Komurov, Vasudha Sehgal, Jiexin Zhang, Lalit Patel, Cristiano G Pereira, Bradley Broom, Gordon B Mills, Prahlad Ram, Paul D Smith, Jennifer A Wargo, Georgina V Long, Michael A Davies

Melanoma Medical Oncology, UT MD Anderson Cancer Center vynanda@mdanderson.org.
2014-10-10; doi: 10.1158/0008-5472.CAN-14-1392
Abstract

Metabolic heterogeneity is a key factor in cancer pathogenesis. We found that a subset of BRAF and NRAS mutant human melanomas resistant to the MEK inhibitor selumetinib displayed increased oxidative phosphorylation (OxPhos) mediated by the transcriptional co-activator PGC1 . Notably, all selumetinib-resistant cells with elevated OxPhos could be re-sensitized by co-treatment with the mTORC1/2 inhibitor AZD8055, whereas this combination was ineffective in resistant cell lines with low OxPhos. In both BRAF- and NRAS-mutant melanoma cells, MEK inhibition increased MITF expression which in turn elevated levels of PGC1 . In contrast, mTORC1/2 inhibition triggered cytoplasmic localization of MITF, decreasing PGC1 expression and inhibiting OxPhos. Analysis of tumor biopsies from BRAF-mutant melanoma patients progressing on BRAF inhibitor ± MEK inhibitor revealed that PGC1 levels were elevated in approximately half of the resistant tumors. Overall, our findings highlight the significance of OxPhos in melanoma and suggest that combined targeting of the MAPK and mTORC pathways may offer an effective therapeutic strategy to treat melanomas with this metabolic phenotype.



Copyright © 2014, American Association for Cancer Research.

PMID:25297634






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