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 …
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 …
[HTML][HTML] LY3009120, a panRAF inhibitor, has significant anti-tumor activity in BRAF and KRAS mutant preclinical models of colorectal cancer
E Vakana, S Pratt, W Blosser, M Dowless, N Simpson… - Oncotarget, 2017 - ncbi.nlm.nih.gov
Activating mutations in the KRAS and BRAF genes, leading to hyperactivation of the
RAS/RAF/MAPK oncogenic signaling cascade, are common in patients with colorectal …
RAS/RAF/MAPK oncogenic signaling cascade, are common in patients with colorectal …
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 …
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 …
Molecular Landscape of Acquired Resistance to Targeted Therapy Combinations in BRAF-Mutant Colorectal Cancer
D Oddo, EM Sennott, L Barault, E Valtorta, S Arena… - Cancer research, 2016 - AACR
Although recent clinical trials of BRAF inhibitor combinations have demonstrated improved
efficacy in BRAF-mutant colorectal cancer, emergence of acquired resistance limits clinical …
efficacy in BRAF-mutant colorectal cancer, emergence of acquired resistance limits clinical …
Development of small-molecule therapeutics and strategies for targeting RAF kinase in BRAF-mutant colorectal cancer
J Pan, H Zhou, S Zhu, J Huang, X Zhao… - Cancer Management …, 2018 - Taylor & Francis
RAF kinase is crucially involved in cell proliferation and survival in colorectal cancer (CRC).
Patients with metastatic CRC (mCRC) harboring BRAF mutations (BRAFms) not only …
Patients with metastatic CRC (mCRC) harboring BRAF mutations (BRAFms) not only …
[HTML][HTML] Therapeutic potential of combined BRAF/MEK blockade in BRAF-wild type preclinical tumor models
A Del Curatolo, F Conciatori, U Cesta Incani… - Journal of Experimental …, 2018 - Springer
Background Mounting evidence suggests that RAF-mediated MEK activation plays a crucial
role in paradox MAPK (re) activation, leading to resistance and therapeutic failure with …
role in paradox MAPK (re) activation, leading to resistance and therapeutic failure with …
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 …
The discovery of exarafenib (KIN-2787): overcoming the challenges of pan-RAF kinase inhibition
YK Chen, T Kanouni, LD Arnold, JM Cox… - Journal of Medicinal …, 2024 - ACS Publications
RAF, a core signaling component of the MAPK kinase cascade, is often mutated in various
cancers, including melanoma, lung, and colorectal cancers. The approved inhibitors were …
cancers, including melanoma, lung, and colorectal cancers. The approved inhibitors were …
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