PIK3CA mutations in advanced cancers: characteristics and outcomes. [PDF]
PIK3CA mutations are frequently diagnosed in diverse cancers and may predict response to PI3K/AKT/mTOR inhibitors. It remains unclear whether they are associated with other characteristics.
Falchook, Gerald S +13 more
core +4 more sources
Allosteric coupling asymmetry mediates paradoxical activation of BRAF by type II inhibitors
The type II class of RAF inhibitors currently in clinical trials paradoxically activate BRAF at subsaturating concentrations. Activation is mediated by induction of BRAF dimers, but why activation rather than inhibition occurs remains unclear.
Damien M Rasmussen +9 more
doaj +1 more source
The treatment of metastatic melanoma is challenging. BRAF gene mutation is found in 40–60% of melanoma cases, the most common being the V600E mutation.
Yu-Ching Weng +5 more
doaj +1 more source
The paradox of cancer genes in non-malignant conditions: implications for precision medicine. [PDF]
Next-generation sequencing has enabled patient selection for targeted drugs, some of which have shown remarkable efficacy in cancers that have the cognate molecular signatures.
Adashek, Jacob J +3 more
core
Co-targeting HGF/cMET Signaling with MEK Inhibitors in Metastatic Uveal Melanoma. [PDF]
Patients with metastatic uveal melanoma usually die within 1 year of diagnosis, emphasizing an urgent need to develop new treatment strategies. The liver is the most common site of metastasis.
Aplin, Andrew E. +8 more
core +2 more sources
Resistant mechanisms to BRAF inhibitors in melanoma [PDF]
Patients with advanced melanoma have traditionally had very poor prognosis. However, since 2011 better understanding of the biology and epidemiology of this disease has revolutionized its treatment, with newer therapies becoming available. These newer therapies can be classified into immunotherapy and targeted therapy.
Manzano, José Luis +6 more
openaire +3 more sources
Mutations of the BRAF gene in human cancer [PDF]
Cancers arise owing to the accumulation of mutations in critical genes that alter normal programmes of cell proliferation, differentiation and death. As the first stage of a systematic genome-wide screen for these genes, we have prioritized for analysis ...
Bignell, G.R. +51 more
core +1 more source
Background The initial use of BRAF targeted therapeutics in clinical trials has demonstrated encouraging responses in melanoma patients, although a rise in drug-resistant cells capable of advancing malignant disease has been described.
Higgins Paul J, Klein R Matthew
doaj +1 more source
ErbB3 Phosphorylation as Central Event in Adaptive Resistance to Targeted Therapy in Metastatic Melanoma. Early Detection in CTCs during Therapy and Insights into Regulation by Autocrine Neuregulin [PDF]
In recent years the introduction of target therapies with BRAF and MEK inhibitors (MAPKi) and of immunotherapy with anti-CTLA-4 and anti-PD-1 monoclonal antibodies have dramatically improved survival of metastatic melanoma patients. Despite these changes
Ascierto, Paolo Antonio +12 more
core +1 more source
Mapping genetic interactions in cancer: a road to rational combination therapies. [PDF]
The discovery of synthetic lethal interactions between poly (ADP-ribose) polymerase (PARP) inhibitors and BRCA genes, which are involved in homologous recombination, led to the approval of PARP inhibition as a monotherapy for patients with BRCA1/2 ...
Krogan, Nevan J, Tutuncuoglu, Beril
core

