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, … MEK2-Q60P
mutation and BRAF gain in a melanoma from a patient who progressed on the MEK inhibitor

MEK inhibitors in the treatment of metastatic melanoma and solid tumors

AM Grimaldi, E Simeone, L Festino, V Vanella… - American journal of …, 2017 - Springer
MEK inhibitor approved for the treatment of BRAF-mutated metastatic melanoma not previously
treated with BRAF inhibitors, … -noncompetitive selective inhibitor of MEK1 and MEK2. In …

MEK inhibitors for the treatment of NRAS mutant melanoma

S Sarkisian, D Davar - Drug Design, Development and Therapy, 2018 - Taylor & Francis
… In this review, we discuss the preclinical data, clinical development, and potential use of
novel MEK inhibitor binemetinib, particularly in the setting of NRAS mutant melanoma. …

Trametinib: a MEK inhibitor for management of metastatic melanoma

I Lugowska, H Koseła-Paterczyk, K Kozak… - OncoTargets and …, 2015 - Taylor & Francis
… Trametinib (Mekinist™) is a reversible and highly selective allosteric inhibitor of MEK1 and
MEK2 with anticancer activity against metastatic melanoma carrying the BRAF V600 mutation

BRAF and MEK inhibition in melanoma

LA Dossett, RR Kudchadkar… - Expert opinion on drug …, 2015 - Taylor & Francis
… -mutant metastatic melanoma. New evidence suggests that the combination of BRAF and
MEK inhibitors … Trametinib is an orally available, potent, selective inhibitor of MEK1 and MEK2

MEK inhibition in the treatment of advanced melanoma

AKS Salama, KB Kim - Current oncology reports, 2013 - Springer
… , non-ATP-competitive inhibitor of both MEK1 and MEK2, was one of the first MEK-targeting
agents to … For NRAS-mutant melanomas, a combination of a MEK inhibitor and a cell cycle …

BRAF and MEK inhibition for the treatment of advanced BRAF mutant melanoma

J Richman, J Martin-Liberal, S Diem… - Expert opinion on …, 2015 - Taylor & Francis
… , dual inhibition of the MAPK pathway with the combination of BRAF and MEK inhibitors in
… In this article, clinical data on dual BRAF and MEK inhibition in advanced melanoma will be …

MEK1 mutations confer resistance to MEK and B-RAF inhibition

CM Emery, KG Vijayendran… - Proceedings of the …, 2009 - National Acad Sciences
… to MEK inhibition, we examined the effects of MEK inhibition on ex vivo melanoma cultures
… for genetic alterations affecting MEK1 (and conceivably MEK2) in cases where resistance …

[HTML][HTML] Resistance to combination BRAF and MEK inhibition in metastatic melanoma: Where to next?

SJ Welsh, H Rizos, RA Scolyer, GV Long - European journal of cancer, 2016 - Elsevier
… For instance, MEK2 mutations are favoured over MEK1 mutations in combination resistant
tumours and BRAF splice variants, which appear to induce low levels of MAPK signalling, are …

[HTML][HTML] Recent advances in the treatment of melanoma with BRAF and MEK inhibitors

E Muñoz-Couselo, JS García… - Annals of …, 2015 - ncbi.nlm.nih.gov
MEK inhibition has emerged as the key component for the treatment of BRAF-mutant metastatic
melanoma… and CRAF), two subtypes of MEK (ME1 and MEK2), and two subtypes of ERK (…