EGFR-Mediated Reactivation of MAPK Signaling Contributes to Insensitivity of BRAF-Mutant Colorectal Cancers to RAF Inhibition with Vemurafenib
RB Corcoran, H Ebi, AB Turke, EM Coffee, M Nishino… - Cancer discovery, 2012 - AACR
BRAF mutations occur in 10% to 15% of colorectal cancers and confer adverse outcome in
the metastatic setting. Although RAF inhibitors such as vemurafenib (PLX4032) have proven …
the metastatic setting. Although RAF inhibitors such as vemurafenib (PLX4032) have proven …
Clinical Acquired Resistance to RAF Inhibitor Combinations in BRAF-Mutant Colorectal Cancer through MAPK Pathway Alterations
LG Ahronian, EM Sennott, EM Van Allen, N Wagle… - Cancer discovery, 2015 - AACR
BRAF mutations occur in approximately 10% of colorectal cancers. Although RAF inhibitor
monotherapy is highly effective in BRAF-mutant melanoma, response rates in BRAF-mutant …
monotherapy is highly effective in BRAF-mutant melanoma, response rates in BRAF-mutant …
BGB-283, a Novel RAF Kinase and EGFR Inhibitor, Displays Potent Antitumor Activity in BRAF-Mutated Colorectal Cancers
Z Tang, X Yuan, R Du, SH Cheung, G Zhang… - Molecular cancer …, 2015 - AACR
Oncogenic BRAF, which drives cell transformation and proliferation, has been detected in
approximately 50% of human malignant melanomas and 5% to 15% of colorectal cancers …
approximately 50% of human malignant melanomas and 5% to 15% of colorectal cancers …
Combined BRAF, EGFR, and MEK Inhibition in Patients with BRAFV600E-Mutant Colorectal Cancer
RB Corcoran, T André, CE Atreya, JHM Schellens… - Cancer discovery, 2018 - AACR
Although BRAF inhibitor monotherapy yields response rates> 50% in BRAF V600-mutant
melanoma, only approximately 5% of patients with BRAF V600E colorectal cancer respond …
melanoma, only approximately 5% of patients with BRAF V600E colorectal cancer respond …
Mechanisms of acquired resistance to BRAF V600E inhibition in colon cancers converge on RAF dimerization and are sensitive to its inhibition
Abstract BRAF V600E colorectal cancers are insensitive to RAF inhibitor monotherapy due
to feedback reactivation of receptor tyrosine kinase signaling. Combined RAF and EGFR …
to feedback reactivation of receptor tyrosine kinase signaling. Combined RAF and EGFR …
Antitumor activity of BRAF inhibitor vemurafenib in preclinical models of BRAF-mutant colorectal cancer
H Yang, B Higgins, K Kolinsky, K Packman… - Cancer research, 2012 - AACR
The protein kinase BRAF is a key component of the RAS–RAF signaling pathway which
plays an important role in regulating cell proliferation, differentiation, and survival. Mutations …
plays an important role in regulating cell proliferation, differentiation, and survival. Mutations …
Combined Pan-RAF and MEK inhibition overcomes multiple resistance mechanisms to selective RAF inhibitors
SR Whittaker, GS Cowley, S Wagner, F Luo… - Molecular cancer …, 2015 - AACR
RAF and MEK inhibitors are effective in BRAF-mutant melanoma but not in BRAF-mutant
colorectal cancer. To gain additional insights into this difference, we performed a genome …
colorectal cancer. To gain additional insights into this difference, we performed a genome …
BRAF Gene Amplification Can Promote Acquired Resistance to MEK Inhibitors in Cancer Cells Harboring the BRAF V600E Mutation
RB Corcoran, D Dias-Santagata, K Bergethon… - Science …, 2010 - science.org
Oncogenic BRAF mutations are found in several tumor types, including melanomas and
colorectal cancers. Tumors with BRAF mutations have increased mitogen-activated protein …
colorectal cancers. Tumors with BRAF mutations have increased mitogen-activated protein …
Concomitant BRAF and PI3K/mTOR Blockade Is Required for Effective Treatment of BRAFV600E Colorectal Cancer
Purpose: BRAFV600E mutations are associated with poor clinical prognosis in colorectal
cancer (CRC). Although selective BRAF inhibitors are effective for treatment of melanoma …
cancer (CRC). Although selective BRAF inhibitors are effective for treatment of melanoma …
Combined BRAF and MEK Inhibition With Dabrafenib and Trametinib in BRAF V600–Mutant Colorectal Cancer
RB Corcoran, CE Atreya, GS Falchook… - Journal of clinical …, 2015 - ascopubs.org
Purpose To evaluate dabrafenib, a selective BRAF inhibitor, combined with trametinib, a
selective MEK inhibitor, in patients with BRAF V600–mutant metastatic colorectal cancer …
selective MEK inhibitor, in patients with BRAF V600–mutant metastatic colorectal cancer …
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