The new platinum(IV) derivative LA-12 shows stronger inhibitory effect on Hsp90 function compared to cisplatin

Result code in IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00209805%3A_____%2F10%3A%230000115" target="_blank" >RIV/00209805:_____/10:#0000115 - isvavai.cz</a>
Result on the web
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DOI - Digital Object Identifier
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Result language
angličtina
Original language name
The new platinum(IV) derivative LA-12 shows stronger inhibitory effect on Hsp90 function compared to cisplatin
Original language description
Cisplatin and its derivatives are commonly used anti-cancer drugs. However, cisplatin has clinical limitations as serious side effects and frequent emergence of resistance. LA-12 shows increased intracellular penetration resulting in improved cytotoxicity in cancer cell lines, including cisplatin resistant cells. LA-12 disrupts cellular proliferation regardless of p53 status, however the potency of the drug is greatly enhanced by the presence of functional p53. Binding of LA-12 to Hsp90 was demonstratedand an inhibitory effect on Hsp90 chaperoning function was shown by decrease of Hsp90-assisted wild-type p53 binding to p21WAF1 promoter sequence in vitro and by accelerated ubiqutination and degradation of primarily unfolded mutant p53 proteins. LA-12induced degradation of Hsp90 client proteins (Cyclin D1 and estrogen receptor) was shown and proved as more efficient compared to cisplatin.
Czech name
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Czech description
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Type
J<sub>x</sub> - Unclassified - Peer-reviewed scientific article (Jimp, Jsc and Jost)
CEP classification
FD - Oncology and haematology
OECD FORD branch
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Project
<a href="/en/project/NS9812" target="_blank" >NS9812: Elucidating the role of ubiquitin-chaperone degradation machinery in cancer and modulating its biochemical functions using targeted chaperone inhibitors</a><br>
Continuities
P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)<br>Z - Vyzkumny zamer (s odkazem do CEZ)

Publication year
2010
Confidentiality
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

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