Reversible and adaptive resistance to BRAF(V600E) inhibition in melanoma

Nature

Volumn 508, Issue 1, 2014, Pages 118-122

  Sun, Chong ^a   Wang, Liqin ^a   Huang, Sidong ^a,b   Heynen, Guus J J E ^a   Prahallad, Anirudh ^a   Robert, Caroline ^c   Haanen, John ^d   Blank, Christian ^d   Wesseling, Jelle ^a   Willems, Stefan M ^a,e   Zecchin, Davide ^f,g   Hobor, Sebastijan ^g   Bajpe, Prashanth K ^a   Lieftink, Cor ^a   Mateus, Christina ^c   Vagner, Stephan ^c   Grernrum, Wipawadee ^a   Hofland, Ingrid ^a   Schlicker, Andreas ^a   Wessels, Lodewyk F A ^a   Beijersbergen, Roderick L ^a   Bardelli, Alberto ^f,g,h   Di Nicolantonio, Federica ^f,g   Eggermont, Alexander M M ^c   Bernards, Rene ^a   more..

^a Cancer Genomics Center Netherlands   (Netherlands)

^b MCGILL UNIVERSITY   (Canada)

^c INSTITUT GUSTAVE ROUSSY   (France)

^d NETHERLANDS CANCER INSTITUTE   (Netherlands)

^e UNIVERSITY MEDICAL CENTER UTRECHT   (Netherlands)

^f UNIVERSITY OF TURIN   (Italy)

^g CANDIOLO CANCER INSTITUTE   (Italy)

^h FIRC INSTITUTE OF MOLECULAR ONCOLOGY   (Italy)

Author keywords

[No Author keywords available]

Indexed keywords

B RAF KINASE; B RAF KINASE INHIBITOR; DABRAFENIB; EPIDERMAL GROWTH FACTOR RECEPTOR; EPIDERMAL GROWTH FACTOR RECEPTOR 3; GEFITINIB; MESSENGER RNA; MITOGEN ACTIVATED PROTEIN KINASE INHIBITOR; PLATELET DERIVED GROWTH FACTOR BETA RECEPTOR; SHORT HAIRPIN RNA; TRAMETINIB; TRANSCRIPTION FACTOR SOX10; TRANSFORMING GROWTH FACTOR BETA; VEMURAFENIB;

ADAPTATION; CANCER; DISEASE TREATMENT; DRUG; GENE EXPRESSION; INHIBITION; INHIBITOR; PUBLIC HEALTH;

ARTICLE; CANCER INHIBITION; CANCER RESISTANCE; HUMAN; HUMAN TISSUE; IN VITRO STUDY; MELANOMA; PHENOTYPE; PRIORITY JOURNAL; PROTEIN EXPRESSION; SIGNAL TRANSDUCTION; UPREGULATION;

ANIMALS; ANTINEOPLASTIC AGENTS; CELL AGING; CELL PROLIFERATION; DRUG RESISTANCE, NEOPLASM; FEMALE; FLOW CYTOMETRY; GENE EXPRESSION REGULATION, NEOPLASTIC; GENE LIBRARY; HUMANS; INDOLES; MELANOMA; MICE; MITOGEN-ACTIVATED PROTEIN KINASE KINASES; PROTEIN KINASE INHIBITORS; PROTO-ONCOGENE PROTEINS B-RAF; RECEPTOR PROTEIN-TYROSINE KINASES; RECEPTOR, EPIDERMAL GROWTH FACTOR; RECEPTOR, PLATELET-DERIVED GROWTH FACTOR BETA; RNA, SMALL INTERFERING; SIGNAL TRANSDUCTION; SOXE TRANSCRIPTION FACTORS; SULFONAMIDES; TRANSFORMING GROWTH FACTOR BETA;

EID: 84897531613     PISSN: 00280836     EISSN: 14764687     Source Type: Journal    
DOI: 10.1038/nature13121     Document Type: Article

References (29)

1. Chapman, P. B. et al. Improved survival with vemurafenib in melanoma with BRAF V600E mutation. N. Engl. J. Med. 364, 2507-2516 (2011).
2. Flaherty, K. T. et al. Improved survival with MEK inhibition in BRAF-mutated melanoma. N. Engl. J. Med. 367, 107-114 (2012).
3. Prahallad, A. et al. Unresponsiveness of colon cancer to BRAF(V600E) inhibition through feedback activation of EGFR. Nature 483, 100-103 (2012).
4. Corcoran, R. B. et al.EGFR-mediated re-activation ofMAPKsignaling contributes to insensitivity ofBRAFmutant colorectal cancers toRAF inhibitionwith vemurafenib. Cancer Discov. 2, 227-235 (2012).
5. Davies, H. et al. Mutations of the BRAF gene in human cancer. Nature 417, 949-954 (2002).
6. Flaherty, K. T., Hodi, F. S.&Fisher, D. E. Fromgenes to drugs: targeted strategies for melanoma. Nature Rev. Cancer 12, 349-361 (2012).
7. Poulikakos, P. I. et al. RAF inhibitor resistance is mediated by dimerization of aberrantly spliced BRAF(V600E). Nature 480, 387-390 (2011).
8. Johannessen, C. M. et al. COT drives resistance to RAF inhibition through MAP kinase pathway reactivation. Nature 468, 968-972 (2010).
9. Wagle, N. et al. Dissecting therapeutic resistance to RAF inhibition inmelanoma by tumour genomic profiling. J. Clin. Oncol. 29, 3085-3096 (2011).
10. Shi, H. et al. Melanoma whole-exome sequencing identifies (V600E)B-RAF amplification-mediated acquired B-RAF inhibitor resistance. Nature Commun. 3, 724 (2012).
11. Nazarian, R. et al. Melanomas acquire resistance to B-RAF(V600E) inhibition by RTK or N-RAS upregulation. Nature 468, 973-977 (2010).
12. Girotti, M. R. et al. Inhibiting EGF receptor or SRC family kinase signaling overcomes BRAF inhibitor resistance in melanoma. Cancer Discov 3, 158-167 (2013).
13. Villanueva, J. et al. Acquired resistance to BRAF inhibitors mediated by a RAF kinase switch in melanoma can be overcome by cotargeting MEK and IGF-1R/PI3K. Cancer Cell 18, 683-695 (2010).
14. Real, F. X. et al. Expression of epidermal growth factor receptor in human cultured cells and tissues: relationship to cell lineage and stage of differentiation. Cancer Res. 46, 4726-4731 (1986).
15. Serrano, M., Lin, A. W., McCurrach, M. E., Beach, D. & Lowe, S. W. Oncogenic ras provokes premature cell senescence associated with accumulation of p53 and p16INK4a. Cell 88, 593-602 (1997).
16. Michaloglou, C. et al. BRAFE600-associated senescence-like cell cycle arrest of human naevi. Nature 436, 720-724 (2005).
17. Brummelkamp, T. R. & Bernards, R. New tools for functional mammalian cancer genetics. Nature Rev. Cancer 3, 781-789 (2003).
18. Huang, S. et al. MED12 controls the response to multiple cancer drugs through regulation of TGF-b receptor signaling. Cell 151, 937-950 (2012).
19. Johnson, A. C. et al. Activator protein-1 mediates induced but not basal epidermal growth factor receptor gene expression. Mol. Med. 6, 17-27 (2000).
20. Zenz, R. et al. c-Jun regulates eyelid closure and skin tumor development through EGFR signaling. Dev. Cell 4, 879-889 (2003).
21. Steller, E. J. et al. PDGFRB promotes liver metastasis formation of mesenchymallike colorectal tumor cells. Neoplasia 15, 204-217 (2013).
22. Zhang, Y., Feng, X.-H.&Derynck, R.Smad3andSmad4cooperate with c-Jun/c-Fos to mediate TGF-b-induced transcription. Nature 394, 909-913 (1998).
23. Mialon, A. et al. DNA topoisomerase I is a cofactor for c-Jun in the regulation of epidermal growth factor receptor expression and cancer cell proliferation. Mol. Cell. Biol. 25, 5040-5051 (2005).
24. Bondurand, N. et al. Interaction among SOX10, PAX3 and MITF, three genes altered in Waardenburg syndrome. Hum. Mol. Genet. 9, 1907-1917 (2000).
25. Garnett, M. J. et al. Systematic identification of genomicmarkers of drug sensitivity in cancer cells. Nature 483, 570-575 (2012).
26. Seghers, A. C., Wilgenhof, S., Lebbe, C. & Neyns, B. Successful rechallenge in two patients with BRAF-V600-mutant melanoma who experienced previous progression during treatment with a selective BRAF inhibitor. Melanoma Res. 22, 466-472 (2012).
27. Yang, X. et al. A public genome-scale lentiviral expression library of humanORFs. Nature Methods 8, 659-661 (2011).
28. Cronin, J. C. et al. Frequentmutations in the MITF pathway inmelanoma. Pigment Cell Melanoma Res 22, 435-444 (2009).
29. Huang, S. et al. ZNF423 is critically required for retinoic acid-induced differentiation and is a marker of neuroblastoma outcome. Cancer Cell 15, 328-340 (2009).