BRAF inhibitor
BRAF Mutant Gastrointestinal Stromal Tumor: First report of regression with BRAF inhibitor dabrafenib (GSK2118436) and whole exomic sequencing for analysis of acquired resistance
... of BRAF have been described in patients with gastrointestinal stromal tumor (GIST), but treatment of GIST with BRAF inhibitors and mechanisms of mediating the emergence of resistance in GIST have not been ...
6
Co clinical assessment identifies patterns of BRAF inhibitor resistance in melanoma
... In this study, we have demonstrated that targeted proteome profil- ing can provide a rapid and cost-effective view of BRAF inhibitor resistance patterns in human melanoma samples. Resistant human samples ...
13
Targeting ER stress–induced autophagy overcomes BRAF inhibitor resistance in melanoma
... of BRAF inhibitor treatment, no significant change was observed in the levels of phospho-AMPK (Thr172; indicating activation) or phospho–p70 S6 kinase (phospho-p70S6K) (Thr308; indicating activation) ...
13
BRAF inhibitor–associated ERK activation drives development of chronic lymphocytic leukemia
... In BRAF WT cells and those with mutations that activate or result in high levels of the BRAF activator RAS, BRAF inhibition can lead to ERK activation, resulting in tumorigenic ...treatment. ...
12
Allele frequencies of BRAF V600 mutations in primary melanomas and matched metastases and their relevance for BRAF inhibitor therapy in metastatic melanoma
... of BRAF inhibitor therapy. BRAF mutations may be detected in archived formalin-fixed, paraffin-embedded (FFPE) melanoma tissue; however, it is currently unclear whether primary tumors, consecutive ...
11
The BRAF Inhibitor Vemurafenib Activates Mitochondrial Metabolism and Inhibits Hyperpolarized Pyruvate-Lactate Exchange in BRAF-Mutant Human Melanoma Cells.
... with BRAF inhibitor treatment, we cannot rule out changes in PC protein expression (resulting from post-transcriptional regulation) or allosteric regulation as potential contributing factors to the elevated ...
35
Therapeutic efficacy of combined BRAF and MEK inhibition in metastatic melanoma: a comprehensive network meta-analysis of randomized controlled trials
... after BRAF inhibition ...mutant BRAF amplification and mutations activating RAS and MEK ...with BRAF V600 mutation and not previously treated with BRAF inhibitors compared with chemotherapy ...
11
Dabrafenib and its potential for the treatment of metastatic melanoma
... Notes: BRAF and NRAS are the most commonly mutated oncogenes in ...to BRAF inhibitor therapy are highlighted in red. BRAF inhibition can lead to activation of the MAPK pathway via acquisition ...
15
PubMedCentral-PMC5726788.pdf
... from BRAF inhibitor relapsed patients and expanded on chronic therapy could be used to identify effective second line combination therapies based on genomic and proteomic profiling (Krepler et ...targeted ...
30
The use of immunotherapy in the treatment of melanoma
... CheckMate 037 was a phase III trial on patients with metastatic melanoma who progressed on or after anti- CTLA-4 therapy and a BRAF inhibitor (if BRAF V600 mutation positive) which demon[r] ...
9
Vemurafenib: a new treatment for BRAF-V600 mutated advanced melanoma
... The BRAF inhibitor, vemurafenib, has demonstrated improved progression-free and overall survival compared with chemotherapy in a randomized trial, and represents a new standard of care in patients with ...
10
Clinical utility of nivolumab in the treatment of advanced melanoma
... with BRAF-mutated disease. Broadly speaking, BRAF/MEK inhibitors offer relatively high response rates, with rapid onset of action (ie, days to weeks), but disease relapse is ...a BRAF ...
13
MEK inhibitors and their potential in the treatment of advanced melanoma: the advantages of combination therapy
... of BRAF inhibitor (vemurafenib and dabrafenib) ...MEK inhibitor (cobimetinib or trametinib), which has proven to increase progression-free survival when compared to BRAF inhibitor ...
10
BRAF inhibitors and radiotherapy for melanoma brain metastases: potential advantages and disadvantages of combination therapy
... activating BRAF mutation, resulting in hyperactive cellular proliferation and ...target BRAF have been introduced for the treatment of metastatic melanoma and offer hope in improving disease outcomes; ...
11
Vemurafenib: an evidence-based review of its clinical utility in the treatment of metastatic melanoma
... to BRAF inhibitors. (c) BRAF amplification and splice ...in BRAF have not been reported, amplification of BRAF as well as activating splice variants have been described in the setting of ...
13
Using quantitative proteomic analysis to understand genotype specific intrinsic drug resistance in melanoma
... In the phase I clinical trial, vemurafenib led to significant levels of tumor shrinkage in 80% of patients whose melanomas harbored the BRAF V600E mutation [20]. This was an unprecedented result for a melanoma ...
7
Development And Characterization Of Novel Raf Dimer Inhibitors To Target Brafv600e Inhibitor Resistance
... Finding BRAF inhibitors that can help bypass inhibitor resistance is crucial in the field of drug discovery due to the strong correlation of BRAF mutation in melanoma, as well as a variety of other ...
181
Mitochondrial oxidative stress is the achille’s heel of melanoma cells resistant to Braf-mutant inhibitor
... of BRAF downstream targets, MEK and ERK, as well as the RTK-dependent stimulation of Akt in vemurafenib-sensitive and derived-resistant sub-lines ...MEK1/2 inhibitor, U0126, indicating that they activated ...
13
Complete response with fluorouracil and irinotecan with a BRAF<sup>V600E</sup> and EGFR inhibitor in BRAF-mutated metastatic colorectal cancer: a case report
... The NGS test results were confirmed from plasma samples with circulating tumor DNA (ctDNA) in a China Food and Drug Administration (CFDA)-approved real-time PCR assay (Super-ARMS EGFR Mutation Detection Kit, Amoy ...
5
Dabrafenib in an elderly patient with metastatic melanoma and BRAF V600R mutation: a case report
... institution, BRAF muta- tions are initially assessed through the cobas 4800 Test and all cases are further confirmed by Sanger sequen- ...with BRAF-mutated MM being treated with dacarbazine in the control ...
5