| GUDERNOVÁ, Iva, Lukáš BÁLEK, Miroslav VAŘECHA, Jana FIALOVÁ KUČEROVÁ, Michaela BOSÁKOVÁ, Bohumil FAFÍLEK, Veronika PALUŠOVÁ, Stjepan ULDRIJAN, Lukáš TRANTÍREK and Pavel KREJČÍ. Inhibitor repurposing reveals ALK, LTK, FGFR, RET and TRK kinases as the targets of AZD1480. Oncotarget. New York: Impact Journals LLC, 2017, vol. 8, No 65, p. 109319-109331. ISSN 1949-2553. Available from: https://dx.doi.org/10.18632/oncotarget.22674. |
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@article{1404487,
author = {Gudernová, Iva and Bálek, Lukáš and Vařecha, Miroslav and Fialová Kučerová, Jana and Bosáková, Michaela and Fafílek, Bohumil and Palušová, Veronika and Uldrijan, Stjepan and Trantírek, Lukáš and Krejčí, Pavel},
article_location = {New York},
article_number = {65},
doi = {http://dx.doi.org/10.18632/oncotarget.22674},
keywords = {AZD1480; drug repurposing; in-cell profiling; inhibitor; receptor tyrosine kinase},
language = {eng},
issn = {1949-2553},
journal = {Oncotarget},
title = {Inhibitor repurposing reveals ALK, LTK, FGFR, RET and TRK kinases as the targets of AZD1480},
url = {http://www.oncotarget.com/index.php?journal=oncotarget&page=article&op=view&path[]=22674&pubmed-linkout=1},
volume = {8},
year = {2017}
}
TY - JOUR
ID - 1404487
AU - Gudernová, Iva - Bálek, Lukáš - Vařecha, Miroslav - Fialová Kučerová, Jana - Bosáková, Michaela - Fafílek, Bohumil - Palušová, Veronika - Uldrijan, Stjepan - Trantírek, Lukáš - Krejčí, Pavel
PY - 2017
TI - Inhibitor repurposing reveals ALK, LTK, FGFR, RET and TRK kinases as the targets of AZD1480
JF - Oncotarget
VL - 8
IS - 65
SP - 109319-109331
EP - 109319-109331
PB - Impact Journals LLC
SN - 19492553
KW - AZD1480
KW - drug repurposing
KW - in-cell profiling
KW - inhibitor
KW - receptor tyrosine kinase
UR - http://www.oncotarget.com/index.php?journal=oncotarget&page=article&op=view&path[]=22674&pubmed-linkout=1
L2 - http://www.oncotarget.com/index.php?journal=oncotarget&page=article&op=view&path[]=22674&pubmed-linkout=1
N2 - Many tyrosine kinase inhibitors (TKIs) have failed to reach human use due to insufficient activity in clinical trials. However, the failed TKIs may still benefit patients if their other kinase targets are identified by providing treatment focused on syndromes driven by these kinases. Here, we searched for novel targets of AZD1480, an inhibitor of JAK2 kinase that recently failed phase two cancer clinical trials due to a lack of activity. Twenty seven human receptor tyrosine kinases (RTKs) and 153 of their disease-associated mutants were in-cell profiled for activity in the presence of AZD1480 using a newly developed RTK plasmid library. We demonstrate that AZD1480 inhibits ALK, LTK, FGFR1-3, RET and TRKA-C kinases and uncover a physical basis of this specificity. The RTK activity profiling described here facilitates inhibitor repurposing by enabling rapid and efficient identification of novel TKI targets in cells.
ER -
GUDERNOVÁ, Iva, Lukáš BÁLEK, Miroslav VAŘECHA, Jana FIALOVÁ KUČEROVÁ, Michaela BOSÁKOVÁ, Bohumil FAFÍLEK, Veronika PALUŠOVÁ, Stjepan ULDRIJAN, Lukáš TRANTÍREK and Pavel KREJČÍ. Inhibitor repurposing reveals ALK, LTK, FGFR, RET and TRK kinases as the targets of AZD1480. \textit{Oncotarget}. New York: Impact Journals LLC, 2017, vol.~8, No~65, p.~109319-109331. ISSN~1949-2553. Available from: https://dx.doi.org/10.18632/oncotarget.22674.
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