Selective BRAFV600E inhibitor PLX4720, requires TRAIL assistance to overcome oncogenic PIK3CA resistance
The result's identifiers
Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F68378050%3A_____%2F11%3A00371716" target="_blank" >RIV/68378050:_____/11:00371716 - isvavai.cz</a>
Result on the web
<a href="http://dx.doi.org/10.1371/journal.pone.0021632" target="_blank" >http://dx.doi.org/10.1371/journal.pone.0021632</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.1371/journal.pone.0021632" target="_blank" >10.1371/journal.pone.0021632</a>
Alternative languages
Result language
angličtina
Original language name
Selective BRAFV600E inhibitor PLX4720, requires TRAIL assistance to overcome oncogenic PIK3CA resistance
Original language description
Documented sensitivity of melanoma cells to PLX4720, a selective BRAFV600E inhibitor, is based on the presence of mutant BRAF(V600E) alone, while wt-BRAF or mutated KRAS result in cell proliferation. In colon cancer BRAF, like KRAS mutations, tend to co-exist with those in PIK3CA. Treatment of two genetically different BRAF(V600E) mutant colon cancer cell lines with BRAF(V600E)inhibitor PLX4720 conferred complete resistance to cell death and TRAIL,an apoptosis inducing agent, was used synergistically inorder to achieve cell death by apoptosis in RKO(BRAFV600E/PIK3CAH1047) cells. For the same level of apoptosis in HT29(BRAFV600E/PIK3CAP449T) cells, TRAIL was combined with 17-AAG, an Hsp90 inhibitor. Pharmacological suppression of the PI3K pathway further enhances the synergistic effect between TRAIL and PLX4720 in RKO cells, indicating the presence of PIK3CA(MT) as the inhibitory factor. Another rational combination includes 17-AAG synergism with TRAIL in a BRAF(V600E) mutant cells.
Czech name
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Czech description
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Classification
Type
J<sub>x</sub> - Unclassified - Peer-reviewed scientific article (Jimp, Jsc and Jost)
CEP classification
EB - Genetics and molecular biology
OECD FORD branch
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Result continuities
Project
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Continuities
Z - Vyzkumny zamer (s odkazem do CEZ)
Others
Publication year
2011
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů
Data specific for result type
Name of the periodical
PLoS ONE
ISSN
1932-6203
e-ISSN
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Volume of the periodical
6
Issue of the periodical within the volume
6
Country of publishing house
US - UNITED STATES
Number of pages
19
Pages from-to
"e21632"
UT code for WoS article
000292092600065
EID of the result in the Scopus database
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