MEK1 mutations confer resistance to MEK and B-RAF inhibition
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Summary
The results affirm the importance of MEK dependency in BRAF-mutant melanoma and suggest novel mechanisms of resistance to MEK and B-RAF inhibitors that may have important clinical implications.
- Type
- article
- Published
- 2009-12-01
- Cited by
- 658
- References
- 31
- Access
- Open access
- OpenAlex
- https://openalex.org/W2009642188
- Semantic Scholar
- https://api.semanticscholar.org/CorpusID:19995327
Keywords
MEK inhibitor, Allosteric regulation, Mutation, Melanoma, Mutagenesis
References
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- Cell signaling and cancer
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- Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling
- Accurate Whole Human Genome Sequencing using Reversible Terminator Chemistry
- Mutation Analysis of BRAF, MEK1 and MEK2 in 15 Ovarian Cancer Cell Lines: Implications for Therapy
- V600EBRAF is associated with disabled feedback inhibition of RAF–MEK signaling and elevated transcriptional output of the pathway
- CI-1040 (PD184352), a targeted signal transduction inhibitor of MEK (MAPKK).
- Structures of human MAP kinase kinase 1 (MEK1) and MEK2 describe novel noncompetitive kinase inhibition
- Nilotinib in imatinib-resistant CML and Philadelphia chromosome-positive ALL.
- Spectrum of MEK1 and MEK2 gene mutations in cardio-facio-cutaneous syndrome and genotype–phenotype correlations
- Mechanisms of autoinhibition and STI-571/imatinib resistance revealed by mutagenesis of BCR-ABL.
- BRAF mutation predicts sensitivity to MEK inhibition
- Addiction to Oncogenes--the Achilles Heal of Cancer
- Modeling genomic diversity and tumor dependency in malignant melanoma.
- Multicenter phase II study of the oral MEK inhibitor, CI-1040, in patients with advanced non-small-cell lung, breast, colon, and pancreatic cancer.
- High-throughput oncogene mutation profiling in human cancer
Cited by
- BRAFV600E Negatively Regulates the AKT Pathway in Melanoma Cell Lines
- Detecting mechanisms of acquired BRAF inhibitor resistance in melanoma.
- Allele-specific mechanisms of activation of MEK1 mutants determine their properties
- Advances in targeted therapy for melanoma.
- New druggable targets in the Ras pathway?
- Whole genome and exome sequencing of melanoma: a step toward personalized targeted therapy.
- The identification of therapeutic targets in metastatic melanoma
- The master-regulators of EMT and E-cadherin constitute a novel pathway in malignant melanoma
- Monoallelic Loss of the Imprinted Gene Grb10 Promotes Tumor Formation in Irradiated Nf1+/- Mice
- Development of malignant melanoma is dependent on a switch in Embryonic Transcription Factors orchestrated by the BRAF-MAPK pathway
- Genomic and Functional Studies of Uveal Melanoma
- Identification of MET and SRC activation in melanoma cell lines showing primary resistance to PLX4032.
- Targeting oncogenic BRAF and aberrant MAPK activation in the treatment of cutaneous melanoma.
- Achievements and challenges of molecular targeted therapy in melanoma.
- Overcoming resistance to BRAF inhibition in BRAF-mutated metastatic melanoma
- Genotyping of cutaneous melanoma
- The role of mitogen‐ and stress‐activated protein kinase pathways in melanoma
- Indução de estresse de retículo endoplasmático como estratégia de quimiossensibilização de melanoma
- Phosphoproteomic Analysis of Cell-Based Resistance to BRAF Inhibitor Therapy in Melanoma
- Preclinical Study of PI3K and BRAF Inhibitors in Malignant Melanoma
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