RAF inhibitors transactivate RAF dimers and ERK signaling in cells with wild-type BRAF
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Summary
Because RAF inhibitors do not inhibit ERK signalling in other cells, the model predicts that they would have a higher therapeutic index and greater antitumour activity than mitogen-activated protein kinase (MEK) inhibitors, but could also cause toxicity due to MEK/ERK activation.
- Type
- article
- Published
- 2010-03-18
- Cited by
- 1,802
- References
- 28
- Access
- Open access
- OpenAlex
- https://openalex.org/W2004295816
- Semantic Scholar
- https://api.semanticscholar.org/CorpusID:2928213
Keywords
Transactivation, MAPK/ERK pathway, Kinase, Vemurafenib, Cancer research
References
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- Regulation and Role of Raf-1/B-Raf Heterodimerization
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- Inhibitor Hijacking of Akt Activation
- Activity of the dual kinase inhibitor lapatinib (GW572016) against HER-2-overexpressing and trastuzumab-treated breast cancer cells.
Cited by
- Rôle de NRAS et PTEN au cours de la mélanomagenèse
- Differential sensitivity of melanoma cell lines with BRAFV600E mutation to the specific Raf inhibitor PLX4032
- Narrative Review: BRAF Opens the Door for Therapeutic Advances in Melanoma
- Clinical characteristics of patients with lung adenocarcinomas harboring BRAF mutations.
- Multiscale Models of Cell Signaling
- BRAFV600E Negatively Regulates the AKT Pathway in Melanoma Cell Lines
- Discovery of a selective kinase inhibitor (TAK-632) targeting pan-RAF inhibition: design, synthesis, and biological evaluation of C-7-substituted 1,3-benzothiazole derivatives.
- Sorafenib sensitizes head and neck squamous cell carcinoma cells to ionizing radiation.
- Somatic activating ARAF mutations in Langerhans cell histiocytosis.
- Epidermal growth factor receptor signalling in keratinocyte biology: implications for skin toxicity of tyrosine kinase inhibitors
- Vemurafenib-induced nonautoimmune haemolytic anaemia.
- Ocular toxicity in BRAF mutant cutaneous melanoma patients treated with vemurafenib.
- New Therapeutic Opportunities Based on DNA Mismatch Repair and BRAF Status in Metastatic Colorectal Cancer
- Phospho-proteomic analyses of B-Raf protein complexes reveal new regulatory principles
- SPRED1 Interferes with K-ras but Not H-ras Membrane Anchorage and Signaling
- Mécanismes de résistances aux inhibiteurs de RAF : revue de la littérature
- Discovery of a novel pan‐RAF inhibitor with potent anti‐tumor activity in preclinical models of BRAFV600E mutant cancer
- Targeting Ras with Macromolecules
- The MEK Inhibitors Trametinib and Cobimetinib Induce a Type I Interferon Response in Human Keratinocytes
- Classifying BRAF alterations in cancer: new rational therapeutic strategies for actionable mutations
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