Targeting the mitogen-activated protein kinase pathway: physiological feedback and drug response
CA Pratilas, DB Solit - Clinical Cancer Research, 2010 - AACR
Mitogen-activated protein kinase (MAPK) pathway activation is a frequent event in human
cancer and is often the result of activating mutations in the BRAF and RAS oncogenes …
cancer and is often the result of activating mutations in the BRAF and RAS oncogenes …
[HTML][HTML] BRAF mutations and the utility of RAF and MEK inhibitors in primary brain tumors
KC Schreck, SA Grossman, CA Pratilas - Cancers, 2019 - mdpi.com
BRAF mutations have been identified as targetable, oncogenic mutations in many cancers.
Given the paucity of treatments for primary brain tumors and the poor prognosis associated …
Given the paucity of treatments for primary brain tumors and the poor prognosis associated …
BRAF mutation predicts sensitivity to MEK inhibition
The kinase pathway comprising RAS, RAF, mitogen-activated protein kinase kinase (MEK)
and extracellular signal regulated kinase (ERK) is activated in most human tumours, often …
and extracellular signal regulated kinase (ERK) is activated in most human tumours, often …
V600EBRAF is associated with disabled feedback inhibition of RAF–MEK signaling and elevated transcriptional output of the pathway
Tumors with mutant BRAF and those with receptor tyrosine kinase (RTK) activation have
similar levels of phosphorylated ERK, but only the former depend on ERK signaling for …
similar levels of phosphorylated ERK, but only the former depend on ERK signaling for …
[PDF][PDF] Relief of profound feedback inhibition of mitogenic signaling by RAF inhibitors attenuates their activity in BRAFV600E melanomas
P Lito, CA Pratilas, EW Joseph, M Tadi, E Halilovic… - Cancer cell, 2012 - cell.com
Summary BRAF V600E drives tumors by dysregulating ERK signaling. In these tumors, we
show that high levels of ERK-dependent negative feedback potently suppress ligand …
show that high levels of ERK-dependent negative feedback potently suppress ligand …
The RAF inhibitor PLX4032 inhibits ERK signaling and tumor cell proliferation in a V600E BRAF-selective manner
EW Joseph, CA Pratilas… - Proceedings of the …, 2010 - National Acad Sciences
Tumors with mutant BRAF and some with mutant RAS are dependent upon ERK signaling
for proliferation, and their growth is suppressed by MAPK/ERK kinase (MEK) inhibitors. In …
for proliferation, and their growth is suppressed by MAPK/ERK kinase (MEK) inhibitors. In …
Loss of NF1 in cutaneous melanoma is associated with RAS activation and MEK dependence
MH Nissan, CA Pratilas, AM Jones, R Ramirez, H Won… - Cancer research, 2014 - AACR
Melanoma is a disease characterized by lesions that activate ERK. Although 70% of
cutaneous melanomas harbor activating mutations in the BRAF and NRAS genes, the …
cutaneous melanomas harbor activating mutations in the BRAF and NRAS genes, the …
Reactivation of ERK signaling causes resistance to EGFR kinase inhibitors
The clinical efficacy of epidermal growth factor receptor (EGFR) kinase inhibitors is limited
by the development of drug resistance. The irreversible EGFR kinase inhibitor WZ4002 is …
by the development of drug resistance. The irreversible EGFR kinase inhibitor WZ4002 is …
Genomic and biological characterization of exon 4 KRAS mutations in human cancer
Mutations in RAS proteins occur widely in human cancer. Prompted by the confirmation of
KRAS mutation as a predictive biomarker of response to epidermal growth factor receptor …
KRAS mutation as a predictive biomarker of response to epidermal growth factor receptor …
Transcriptional pathway signatures predict MEK addiction and response to selumetinib (AZD6244)
Abstract Selumetinib (AZD6244, ARRY-142886) is a selective, non–ATP-competitive
inhibitor of mitogen-activated protein/extracellular signal–regulated kinase kinase (MEK) …
inhibitor of mitogen-activated protein/extracellular signal–regulated kinase kinase (MEK) …