Thursday, August 9, 2012
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Assays & screens
Impact of receptor tyrosine kinase (RTK) ligands on sensitivity
of human tumor-derived cell lines to kinase inhibitors
Analysis of the impact of
RTK ligands on sensitivity of human tumor-derived cell lines to kinase inhibitors
could guide combination therapy to prevent drug resistance. In about half of BRAF mutant melanoma cell lines, the RTK ligand hepatocyte growth factor/scatter factor
(HGF/SF) induced c-Met proto-oncogene (MET;
HGFR) expression and
resistance to the BRAF inhibitor Zelboraf vemurafenib. In
these cell lines, co-treatment with the MET kinase inhibitorXalkori crizotinib
prevented resistance to Zelboraf. In patients with BRAF mutant melanoma, increased plasma HGF/SF levels
correlated with poorer survival outcomes than normal HGF/SF levels. Next
steps include analyzing the effects of RTK ligands on larger numbers of
kinase-activated, human tumor-derived cell lines.
Zelboraf, from Daiichi Sankyo Co. Ltd., Chugai Pharmaceutical Co. Ltd.
and Roche, is marketed to treat
melanoma, in Phase I testing for colorectal cancer and in Phase II testing
for thyroid cancer.
Xalkori from Pfizer Inc., which also
inhibits anaplastic lymphoma kinase
(ALK), is marketed to treat
non-small cell lung cancer (NSCLC) and is in Phase I testing to treat solid
SciBX 5(31); doi:10.1038/scibx.2012.825
Published online Aug. 9, 2012
Patent and licensing status
Wilson, T.R. et al. Nature; published online July 4, 2012;
Contact: Jeffrey Settleman, Genentech Inc., South San
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