Thursday, August 8, 2013
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Assays & screens
Assay for profiling kinase
inhibitor-target interaction in cells
In vitro and cell culture studies suggest an assay for
monitoring kinase inhibitor-sensitive chaperone-kinase interactions could
help identify targets of kinase inhibitors in cells. In vitro, luciferase-tagged
protein 90 (Hsp90)
directly bound to BCR-ABL
tyrosine kinase, producing a luminescent signal in the
assay. In this assay, the nonselective BCR-ABL inhibitor Gleevec
decreased both Hsp90 binding to BCR-ABL and luminescent signal compared with
no treatment. The assay showed that a panel of inhibitors selectively blocked
kinase-chaperone interactions in a manner consistent with known specificities
and identified neurotrophic
tyrosine kinase receptor 3 (NTRK3;
as an additional target of Xalkori
Next steps include testing Xalkori in models for tumors caused by NTRK3
mutations, including fibrosarcomas.
AG markets Gleevec to treat chronic myelogenous leukemia
(CML) and gastrointestinal stromal tumors.
Inc. markets Xalkori, a dual inhibitor of c-Met
receptor tyrosine kinase and anaplastic
lymphoma kinase (ALK),
to treat non-small cell lung cancer (NSCLC).
Published online Aug. 8, 2013
Patent pending; available
Taipale, M. et al. Nat.
Biotechnol.; published online June 30, 2013;
Contact: Susan Lindquist, Whitehead Institute for Biomedical
Research, Cambridge, Mass.
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