Incidence of the V600K mutation among melanoma patients with BRAF mutations, and potential therapeutic response to the specific BRAF inhibitor PLX4032
Top Cited Papers
Open Access
- 14 July 2010
- journal article
- Published by Springer Nature in Journal of Translational Medicine
- Vol. 8 (1) , 67
- https://doi.org/10.1186/1479-5876-8-67
Abstract
Activating mutations in BRAF kinase are common in melanomas. Clinical trials with PLX4032, the mutant-BRAF inhibitor, show promising preliminary results in patients selected for the presence of V600E mutation. However, activating V600K mutation is the other most common mutation, yet patients with this variant are currently excluded from the PLX4032 trials. Here we present evidence that a patient bearing the BRAF V600K mutation responded remarkably to PLX4032, suggesting that clinical trials should include all patients with activating BRAF V600E/K mutations.Keywords
This publication has 11 references indexed in Scilit:
- Targeting the Mitogen-Activated Protein Kinase Pathway: Physiological Feedback and Drug ResponseClinical Cancer Research, 2010
- PLX4032, a selective BRAF V600E kinase inhibitor, activates the ERK pathway and enhances cell migration and proliferation of BRAF WT melanoma cellsPigment Cell & Melanoma Research, 2010
- Phase I study of PLX4032: Proof of concept for V600E BRAF mutation as a therapeutic target in human cancerJournal of Clinical Oncology, 2009
- BRAF Silencing by Short Hairpin RNA or Chemical Blockade by PLX4032 Leads to Different Responses in Melanoma and Thyroid Carcinoma CellsMolecular Cancer Research, 2008
- Application of a BRAF Pyrosequencing Assay for Mutation Detection and Copy Number Analysis in Malignant MelanomaThe Journal of Molecular Diagnostics, 2007
- BRAF mutations in melanocytic lesions and papillary thyroid carcinoma samples identified using melting curve analysis of polymerase chain reaction products.Archives of Pathology & Laboratory Medicine, 2007
- B-RAF and N-RAS Mutations Are Preserved during Short Time In Vitro Propagation and Differentially Impact PrognosisPLOS ONE, 2007
- BRAF and NRAS mutations in melanoma and melanocytic neviMelanoma Research, 2006
- Human malignant melanoma: detection of BRAF- and c-kit–activating mutations by high-resolution amplicon melting analysisHuman Pathology, 2005
- BRAF MutationThe American Journal of Dermatopathology, 2003