The DOI matches its Crossref record; 4 of the 4 references it cites were found in a registry or an index.
Differential sensitivity of melanoma cell lines with BRAF V600E mutation to the specific Raf inhibitor PLX4032
Open accessAbstract
Blocking oncogenic signaling induced by the BRAF V600E mutation is a promising approach for melanoma treatment. We tested the anti-tumor effects of a specific inhibitor of Raf protein kinases, PLX4032/RG7204, in melanoma cell lines. PLX4032 decreased signaling through the MAPK pathway only in cell lines with the BRAF V600E mutation. Seven out of 10 BRAF V600E mutant cell lines displayed sensitivity based on cell viability assays and three were resistant at concentrations up to 10 μM. Among the sensitive cell lines, four were highly sensitive with IC 50 values below 1 μM, and three were moderately sensitive with IC 50 values between 1 and 10 μM. There was evidence of MAPK pathway inhibition and cell cycle arrest in both sensitive and resistant cell lines. Genomic analysis by sequencing, genotyping of close to 400 oncogeninc mutations by mass spectrometry, and SNP arrays demonstrated no major differences in BRAF locus amplification or in other oncogenic events between sensitive and resistant cell lines. However, metabolic tracer uptake studies demonstrated that sensitive cell lines had a more profound inhibition of FDG uptake upon exposure to PLX4032 than resistant cell lines. In conclusion, BRAF V600E mutant melanoma cell lines displayed a range of sensitivities to PLX4032 and metabolic imaging using PET probes can be used to assess sensitivity.
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Cites
Mutations of the BRAF gene in human cancer
Davies, H., Bignell, G. R., Cox, C., Stephens, P., Edkins, S., Clegg, S., Teague, J., Woffendin, H., Garnett, M. J., Bottomley, W., et al. (2002) · Nature · doi:10.1038/nature00766 · Cited by 10,674
Wang, K., Li, M., Hadley, D., Liu, R., Glessner, J., Grant, S. F. A., Hakonarson, H., & Bucan, M. (2007) · Genome Research · doi:10.1101/gr.6861907 · Cited by 1,792
Melanoma biology and new targeted therapy
Gray-Schopfer, V., Wellbrock, C., & Marais, R. (2007) · Nature · doi:10.1038/nature05661 · Cited by 1,371
Friday, B. B., Yu, C., Dy, G. K., Smith, P. D., Wang, L., Thibodeau, S. N., & Adjei, A. A. (2008) · Cancer Research · doi:10.1158/0008-5472.can-08-1430 · Cited by 146
Cited by
Inhibition of Mutated, Activated BRAF in Metastatic Melanoma
Flaherty, K. T., Puzanov, I., Kim, K. B., Ribas, A., McArthur, G. A., Sosman, J. A., O'Dwyer, P. J., Lee, R. J., Grippo, J. F., Nolop, K., et al. (2010) · New England Journal of Medicine · doi:10.1056/nejmoa1002011 · Cited by 3,103
Self-citationSurvival in BRAF V600-mutant advanced melanoma treated with vemurafenib
Sosman, J. A., Kim, K. B., Schuchter, L., Gonzalez, R., Pavlick, A. C., Weber, J. S., McArthur, G. A., Hutson, T. E., Moschos, S. J., Flaherty, K. T., et al. (2012) · New England Journal of Medicine · doi:10.1056/nejmoa1112302 · Cited by 2,156
Self-citationTsoi, J., Robert, L., Paraiso, K., Galvan, C., Sheu, K. M., Lay, J., Wong, D. J. L., Atefi, M., Shirazi, R., Wang, X., et al. (2018) · Cancer Cell · doi:10.1016/j.ccell.2018.03.017 · Cited by 938
Self-citationGrasso, C. S., Tsoi, J., Onyshchenko, M., Abril-Rodriguez, G., Ross-Macdonald, P., Wind-Rotolo, M., Champhekar, A., Medina, E., Torrejon, D. Y., Shin, D. S., et al. (2020) · Cancer Cell · doi:10.1016/j.ccell.2020.08.005 · Cited by 390
Self-citationRaf Family Kinases: Old Dogs Have Learned New Tricks
Matallanas, D., Birtwistle, M., Romano, D., Zebisch, A., Rauch, J., von Kriegsheim, A., & Kolch, W. (2011) · Genes & Cancer · doi:10.1177/1947601911407323 · Cited by 386
Metadata
- Authors
- Søndergaard, J. N., Nazarian, R., Wang, Q., Guo, D., Hsueh, T., Mok, S., Sazegar, H., MacConaill, L. E., Barretina, J. G., Kehoe, S. M., Attar, N., von Euw, E., Zuckerman, J. E., Chmielowski, B., Comin-Anduix, B., Koya, R. C., Mischel, P. S., Lo, R. S., & Ribas, A.
- Venue
- Journal of Translational Medicine
- Published
- 2010-04-20
- Volume
- 8
- Issue
- 1
- Pages
- 39-39
- ISSN
- 1479-5876 (ISSN-L)
- OpenAlex
- W2108537717
- Cited by
- 228
- References
- 4
- FWCI
- 9.81
- Type
- journal article
- Language
- en
- Open access
- gold
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- The paper
- Søndergaard, J. N., Nazarian, R., Wang, Q., Guo, D., Hsueh, T., Mok, S., Sazegar, H., MacConaill, L. E., Barretina, J. G., Kehoe, S. M., Attar, N., von Euw, E., Zuckerman, J. E., Chmielowski, B., Comin-Anduix, B., Koya, R. C., Mischel, P. S., Lo, R. S., & Ribas, A. (2010). Differential sensitivity of melanoma cell lines with BRAF V600E mutation to the specific Raf inhibitor PLX4032. Journal of Translational Medicine. https://doi.org/10.1186/1479-5876-8-39
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Bibliographic data: Semantic Scholar, OpenAlex, Crossref.
Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.
