Preexisting MEK1P124 mutations diminish response to BRAF inhibitors in metastatic melanoma patients

Clinical Cancer Research

Volumn 21, Issue 1, 2015, Pages 98-105

  Carlino, Matteo S ^a,b,c   Fung, Carina ^a,d   Shahheydari, Hamideh ^d   Todd, Jason R ^a   Boyd, Suzanah C ^d   Irvine, Mal ^d   Nagrial, Adnan M ^e   Scolyer, Richard A ^c,f,g   Kefford, Richard F ^a,d,f   Long, Georgina V ^c,f   Rizos, Helen ^a,d,f  

^a WESTMEAD HOSPITAL   (Australia)

^b BLACKTOWN HOSPITAL   (Australia)

^c MELANOMA INSTITUTE AUSTRALIA   (Australia)

^d MACQUARIE UNIVERSITY   (Australia)

^e GARVAN INSTITUTE OF MEDICAL RESEARCH   (Australia)

^f UNIVERSITY OF SYDNEY   (Australia)

^g ROYAL PRINCE ALFRED HOSPITAL   (Australia)

Author keywords

[No Author keywords available]

Indexed keywords

DABRAFENIB; MITOGEN ACTIVATED PROTEIN KINASE; MITOGEN ACTIVATED PROTEIN KINASE KINASE 1; PROLINE; VEMURAFENIB; B RAF KINASE; BRAF PROTEIN, HUMAN; IMIDAZOLE DERIVATIVE; INDOLE DERIVATIVE; MAP2K1 PROTEIN, HUMAN; OXIME; SULFONAMIDE;

ARTICLE; BRAF GENE; CANCER COMBINATION CHEMOTHERAPY; CHEMOSENSITIVITY; CONTROLLED STUDY; CORRELATIONAL STUDY; DRUG RESPONSE; ENZYME ACTIVITY; ENZYME INHIBITION; GENE MUTATION; GENOTYPE; HUMAN; HUMAN CELL; HUMAN TISSUE; MAJOR CLINICAL STUDY; MEK1 GENE; MELANOMA CELL LINE; METASTATIC MELANOMA; MUTANT; ONCOGENE; PHASE 2 CLINICAL TRIAL (TOPIC); PROGRESSION FREE SURVIVAL; PROTEIN PHOSPHORYLATION; SIGNAL TRANSDUCTION; WILD TYPE; ANTAGONISTS AND INHIBITORS; DISEASE FREE SURVIVAL; DRUG RESISTANCE; GENETICS; MELANOMA; MUTATION; PATHOLOGY;

DISEASE-FREE SURVIVAL; DRUG RESISTANCE, NEOPLASM; HUMANS; IMIDAZOLES; INDOLES; MAP KINASE KINASE 1; MELANOMA; MUTATION; OXIMES; PROTO-ONCOGENE PROTEINS B-RAF; SULFONAMIDES;

EID: 84920670424     PISSN: 10780432     EISSN: 15573265     Source Type: Journal    
DOI: 10.1158/1078-0432.CCR-14-0759     Document Type: Article

References (40)

1. Flaherty KT, Puzanov I, Kim KB, Ribas A, McArthur GA, Sosman JA, et al. Inhibition of mutated, activated BRAF in metastatic melanoma. N Engl J Med 2010;363:809-19.
2. Chapman PB, Hauschild A, Robert C, Haanen JB, Ascierto P, Larkin J, et al. Improved survival with vemurafenib in melanoma with BRAF V600E mutation. N Engl J Med 2011;364:2507-16.
3. Falchook GS, Long GV, Kurzrock R, Kim KB, Arkenau TH, Brown MP, et al. Dabrafenib in patients with melanoma, untreated brain metastases, and other solid tumours: a phase 1 dose-escalation trial. Lancet 2012;379:1893-901.
4. Hauschild A, Grob J-J, Demidov LV, Jouary T, Gutzmer R, Millward M, et al. Dabrafenib in BRAF-mutated metastatic melanoma: a multicentre, openlabel, phase 3 randomised controlled trial. Lancet 2012;380:358-65.
5. Montagut C, Sharma SV, Shioda T, McDermott U, Ulman M, Ulkus LE, et al. Elevated CRAF as a potential mechanism of acquired resistance to BRAF inhibition in melanoma. Cancer Res 2008;68:4853-61.
6. Johannessen CM, Boehm JS, Kim SY, Thomas SR, Wardwell L, Johnson LA, et al. COT drives resistance to RAF inhibition through MAP kinase pathway reactivation. Nature 2010;468:968-72.
7. Shi H, Moriceau G, Kong X, Lee M-K, Lee H, Koya RC, et al. Melanoma whole-exome sequencing identifies V600EB-RAF amplification-mediated acquired B-RAF inhibitor resistance. Nat Commun 2012;3:724.
8. Poulikakos PI, Persaud Y, Janakiraman M, Kong X, Ng C, Moriceau G, et al. RAF inhibitor resistance is mediated by dimerization of aberrantly spliced BRAF(V600E). Nature 2011;480:387-90.
9. Nazarian R, Shi H, Wang Q, Kong X, Koya RC, Lee H, et al. Melanomas acquire resistance to B-RAF(V600E) inhibition by RTK or N-RAS upregulation. Nature 2010;468:973-7.
10. Watson IR, Li L, Cabeceiras PK, Mahdavi M, Gutschner T, Genovese G, et al. The RAC1 P29S hotspot mutation in melanoma confers resistance to pharmacological inhibition of RAF. Cancer Res 2014;74:4845-52.
11. Whittaker SR, Theurillat JP, Van Allen E, Wagle N, Hsiao J, Cowley GS, et al. Agenome-scale RNA interference screen implicates NF1 loss in resistance to RAF inhibition. Cancer Discov 2013;3:350-62.
12. Villanueva J, Vultur A, Lee JT, Somasundaram R, Fukunaga-Kalabis M, Cipolla AK, 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 2010;18:683-95.
13. Girotti MR, Pedersen M, Sanchez-Laorden B, Viros A, Turajlic S, Niculescu-Duvaz D, et al. Inhibiting EGF receptor or SRC family kinase signaling overcomes BRAF inhibitor resistance in melanoma. Cancer Discov 2013;3:158-67.
14. Van Allen EM, Wagle N, Sucker A, Treacy DJ, Johannessen CM, Goetz EM, et al. The genetic landscape of clinical resistance to RAF inhibition in metastatic melanoma. Cancer Discov 2014;4:94-109.
15. Shi H, Hong A, Kong X, Koya RC, Song C, Moriceau G, et al. A novel AKT1 mutant amplifies an adaptive melanoma response to BRAF inhibition. Cancer Discov 2014;4:69-79.
16. Shi H, Hugo W, Kong X, Hong A, Koya RC, Moriceau G, et al. Acquired resistance and clonal evolution in melanoma during BRAF inhibitor therapy. Cancer Discov 2014;4:80-93.
17. Nathanson KL, Martin AM, Wubbenhorst B, Greshock J, Letrero R, D'Andrea K, et al. Tumor genetic analyses of patients with metastatic melanoma treated with the BRAF inhibitor dabrafenib (GSK2118436). Clin Cancer Res 2013;19:4868-78.
18. Sondergaard JN, Nazarian R, Wang Q, Guo D, Hsueh T, Mok S, et al. Differential sensitivity of melanoma cell lines with BRAFV600E mutation to the specific Raf inhibitor PLX4032. J Transl Med 2010;8:39.
19. Trunzer K, Pavlick AC, Schuchter L, Gonzalez R, McArthur GA, Hutson TE, et al. Pharmacodynamic effects and mechanisms of resistance to vemurafenib in patients with metastatic melanoma. J Clin Oncol 2013;31:1767-74.
20. Emery CM, Vijayendran KG, Zipser MC, Sawyer AM, Niu L, Kim JJ, et al. MEK1 mutations confer resistance to MEK and B-RAF inhibition. Proc Natl Acad Sci U S A 2009;106:20411-6.
21. Wagle N, Emery C, Berger MF, Davis MJ, Sawyer A, Pochanard P, et al. Dissecting therapeutic resistance to RAF inhibition inmelanoma by tumor genomic profiling. J Clin Oncol 2011;29:3085-96.
22. Rizos H, Menzies AM, Pupo GM, Carlino MS, Fung C, Hyman J, et al. BRAF inhibitor resistance mechanisms in metastatic melanoma: spectrum and clinical impact. Clin Cancer Res 2014;20:1965-77.
23. Hodis E, Watson Ian R, Kryukov Gregory V, Arold Stefan T, Imielinski M, Theurillat J-P, et al. A landscape of driver mutations in melanoma. Cell 2012;150:251-63.
24. Shi H, Moriceau G, Kong X, Koya RC, Nazarian R, Pupo GM, et al. Preexisting MEK1 exon 3 mutations in V600E/KBRAF melanomas do not confer resistance to BRAF inhibitors. Cancer Discov 2012;2:414-24.
25. Nikolaev SI, Rimoldi D, Iseli C, Valsesia A, Robyr D, Gehrig C, et al. Exome sequencing identifies recurrent somatic MAP2K1 and MAP2K2 mutations in melanoma. Nat Genet 2011;44:133-9.
26. Allanson JE, Anneren G, Aoki Y, Armour CM, Bondeson ML, Cave H, et al. Cardio-facio-cutaneous syndrome: does genotype predict phenotype? Am J Med Genet C Semin Med Genet 2011;157C:129-35.
27. Sosman JA, Kim KB, Schuchter L, Gonzalez R, Pavlick AC, Weber JS, et al. Survival in BRAF V600-mutant advanced melanoma treated with vemurafenib. N Engl J Med 2012;366:707-14.
28. Carlino MS, Gowrishankar K, Saunders CAB, Pupo GM, Snoyman S, Zhang XD, et al. Antiproliferative effects of continued mitogen-activated protein kinase pathway inhibition following acquired resistance to BRAF and/or MEK inhibition in melanoma. Mol Cancer Ther 2013;12:1332-42.
29. Carlino MS, Todd JR, Gowrishankar K, Mijatov B, Pupo GM, Fung C, et al. Differential activity of MEK and ERK inhibitors in BRAF inhibitor resistant melanoma. Mol Oncol 2014;8:544-54.
30. Haferkamp S, Scurr LL, Becker TM, Frausto M, Kefford RF, Rizos H. Oncogene-induced senescence does not require the p16INK4a or p14ARF melanoma tumor suppressors. J Inv Dermatol 2009;129:1983-91.
31. Catalogue of somatic mutations in cancer (COSMIC) website. Available from: http://cancer.sanger.ac.uk/cancergenome/projects/cosmic/: Wellcome Trust Sanger Institute.
32. Greenman C, Stephens P, Smith R, Dalgliesh GL, Hunter C, Bignell G, et al. Patterns of somatic mutation in human cancer genomes. Nature 2007;446:153-8.
33. Fischmann TO, Smith CK, Mayhood TW, Myers JE, Reichert P, Mannarino A, et al. Crystal structures of MEK1 binary and ternary complexes with nucleotides and inhibitors. Biochemistry 2009;48:2661-74.
34. Dutton-Regester K, Irwin D, Hunt P, Aoude LG, Tembe V, Pupo GM, et al. A high-throughput panel for identifying clinically relevant mutation profiles in melanoma. Mol Cancer Ther 2012;11:888-97.
35. Flaherty KT, Infante JR, Daud A, Gonzalez R, Kefford RF, Sosman J, et al. Combined BRAF and MEK inhibition in melanoma with BRAF V600 mutations. N Engl J Med 2012;367:1694-703.
36. Ascierto PA, Minor D, Ribas A, Lebbe C, O'Hagan A, Arya N, et al. Phase II trial (BREAK-2) of the BRAF inhibitor dabrafenib (GSK2118436) in patients with metastatic melanoma. J Clin Oncol 2013;31:3205-11.
37. Carlino MS, Saunders CA, Haydu LE, Menzies AM, Martin Curtis C Jr, Lebowitz PF, et al. (18)F-labelled fl uorodeoxyglucose-positron emission tomography (FDG-PET) heterogeneity of response is prognostic in dabrafenib treated BRAF mutant metastatic melanoma. Eur J Cancer 2013;49:395-402.
38. Stones CJ, Kim JE, Joseph WR, Leung E, Marshall ES, Finlay GJ, et al. Comparison of responses of human melanoma cell lines to MEK and BRAF inhibitors. Front genet 2013;4:66.
39. Halaban R, Zhang W, Bacchiocchi A, Cheng E, Parisi F, Ariyan S, et al. PLX4032, a selective BRAF(V600E) kinase inhibitor, activates the ERK pathway and enhances cell migration and proliferation of BRAF melanoma cells. Pigment Cell Melanoma Res 2010;23:190-200.
40. King AJ, Arnone MR, Bleam MR, Moss KG, Yang J, Fedorowicz KE, et al. Dabrafenib; preclinical characterization, increased efficacy when combined with trametinib, while BRAF/MEK tool combination reduced skin lesions. PLoS ONE 2013;8:e67583.