[HTML][HTML] Increased MAPK reactivation in early resistance to dabrafenib/trametinib combination therapy of BRAF-mutant metastatic melanoma
GV Long, C Fung, AM Menzies, GM Pupo… - Nature …, 2014 - nature.com
One-third of BRAF-mutant metastatic melanoma patients treated with combined BRAF and
MEK inhibition progress within 6 months. Treatment options for these patients remain …
MEK inhibition progress within 6 months. Treatment options for these patients remain …
MAP Kinase Pathway Alterations in BRAF-Mutant Melanoma Patients with Acquired Resistance to Combined RAF/MEK Inhibition
Abstract Treatment of BRAF-mutant melanoma with combined dabrafenib and trametinib,
which target RAF and the downstream MAP–ERK kinase (MEK) 1 and MEK2 kinases …
which target RAF and the downstream MAP–ERK kinase (MEK) 1 and MEK2 kinases …
[HTML][HTML] Concurrent MEK2 mutation and BRAF amplification confer resistance to BRAF and MEK inhibitors in melanoma
J Villanueva, JR Infante, C Krepler, P Reyes-Uribe… - Cell reports, 2013 - cell.com
Although BRAF and MEK inhibitors have proven clinical benefits in melanoma, most patients
develop resistance. We report a de novo MEK2-Q60P mutation and BRAF gain in a …
develop resistance. We report a de novo MEK2-Q60P mutation and BRAF gain in a …
Preexisting MEK1P124 Mutations Diminish Response to BRAF Inhibitors in Metastatic Melanoma Patients
MS Carlino, C Fung, H Shahheydari, JR Todd… - Clinical Cancer …, 2015 - AACR
Background: MEK1 mutations in melanoma can confer resistance to BRAF inhibitors,
although preexisting MEK1P124 mutations do not preclude clinical responses. We sought to …
although preexisting MEK1P124 mutations do not preclude clinical responses. We sought to …
The genetic landscape of clinical resistance to RAF inhibition in metastatic melanoma
EM Van Allen, N Wagle, A Sucker, DJ Treacy… - Cancer discovery, 2014 - AACR
Most patients with BRAF V600-mutant metastatic melanoma develop resistance to selective
RAF kinase inhibitors. The spectrum of clinical genetic resistance mechanisms to RAF …
RAF kinase inhibitors. The spectrum of clinical genetic resistance mechanisms to RAF …
PAK signalling drives acquired drug resistance to MAPK inhibitors in BRAF-mutant melanomas
Targeted BRAF inhibition (BRAFi) and combined BRAF and MEK inhibition (BRAFi and
MEKi) therapies have markedly improved the clinical outcomes of patients with metastatic …
MEKi) therapies have markedly improved the clinical outcomes of patients with metastatic …
[HTML][HTML] Resistance to BRAF-targeted therapy in melanoma
RJ Sullivan, KT Flaherty - European journal of cancer, 2013 - Elsevier
BRAF mutations are identified in 40–50% of patients with melanoma. Treatment of these
patients with either of two BRAF inhibitors (vemurafenib, dabrafenib) or the MEK inhibitor …
patients with either of two BRAF inhibitors (vemurafenib, dabrafenib) or the MEK inhibitor …
Preexisting MEK1 Exon 3 Mutations in V600E/KBRAF Melanomas Do Not Confer Resistance to BRAF Inhibitors
H Shi, G Moriceau, X Kong, RC Koya, R Nazarian… - Cancer discovery, 2012 - AACR
BRAF inhibitors (BRAFi) induce antitumor responses in nearly 60% of patients with
advanced V600E/K BRAF melanomas. Somatic activating MEK1 mutations are thought to be …
advanced V600E/K BRAF melanomas. Somatic activating MEK1 mutations are thought to be …
[HTML][HTML] Effects of AKT inhibitor therapy in response and resistance to BRAF inhibition in melanoma
A Lassen, M Atefi, L Robert, DJL Wong, M Cerniglia… - Molecular cancer, 2014 - Springer
Background The clinical use of BRAF inhibitors for treatment of metastatic melanoma is
limited by the development of drug resistance. In this study we investigated whether co …
limited by the development of drug resistance. In this study we investigated whether co …
[HTML][HTML] Reversing melanoma cross-resistance to BRAF and MEK inhibitors by co-targeting the AKT/mTOR pathway
Background The sustained clinical activity of the BRAF inhibitor vemurafenib
(PLX4032/RG7204) in patients with BRAFV600 mutant melanoma is limited primarily by the …
(PLX4032/RG7204) in patients with BRAFV600 mutant melanoma is limited primarily by the …
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