Inhibitor repurposing reveals ALK, LTK, FGFR, RET and TRK kinases as the targets of AZD1480
The result's identifiers
Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00159816%3A_____%2F17%3A00068379" target="_blank" >RIV/00159816:_____/17:00068379 - isvavai.cz</a>
Alternative codes found
RIV/00216224:14110/17:00095429
Result on the web
<a href="http://www.oncotarget.com/index.php?journal=oncotarget&page=article&op=view&path" target="_blank" >http://www.oncotarget.com/index.php?journal=oncotarget&page=article&op=view&path</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.18632/oncotarget.22674" target="_blank" >10.18632/oncotarget.22674</a>
Alternative languages
Result language
angličtina
Original language name
Inhibitor repurposing reveals ALK, LTK, FGFR, RET and TRK kinases as the targets of AZD1480
Original language description
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.
Czech name
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Czech description
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Classification
Type
J<sub>imp</sub> - Article in a specialist periodical, which is included in the Web of Science database
CEP classification
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OECD FORD branch
30204 - Oncology
Result continuities
Project
Result was created during the realization of more than one project. More information in the Projects tab.
Continuities
P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)
Others
Publication year
2017
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů
Data specific for result type
Name of the periodical
Oncotarget
ISSN
1949-2553
e-ISSN
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Volume of the periodical
8
Issue of the periodical within the volume
65
Country of publishing house
US - UNITED STATES
Number of pages
13
Pages from-to
109319-109331
UT code for WoS article
000419565400082
EID of the result in the Scopus database
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