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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 demonstrated and 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-12 induced degradation of Hsp90 client proteins (Cyclin D1 and estrogen receptor) was shown and proved as more efficient compared to cisplatin.
- 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 demonstrated and 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-12 induced degradation of Hsp90 client proteins (Cyclin D1 and estrogen receptor) was shown and proved as more efficient compared to cisplatin. (en)
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Title
| - The new platinum(IV) derivative LA-12 shows stronger inhibitory effect on Hsp90 function compared to cisplatin
- The new platinum(IV) derivative LA-12 shows stronger inhibitory effect on Hsp90 function compared to cisplatin (en)
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skos:prefLabel
| - The new platinum(IV) derivative LA-12 shows stronger inhibitory effect on Hsp90 function compared to cisplatin
- The new platinum(IV) derivative LA-12 shows stronger inhibitory effect on Hsp90 function compared to cisplatin (en)
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skos:notation
| - RIV/00209805:_____/10:#0000115!RIV11-MZ0-00209805
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http://linked.open...avai/riv/aktivita
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http://linked.open...avai/riv/aktivity
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http://linked.open...iv/cisloPeriodika
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http://linked.open...vai/riv/dodaniDat
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http://linked.open...aciTvurceVysledku
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http://linked.open.../riv/druhVysledku
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http://linked.open...iv/duvernostUdaju
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http://linked.open...titaPredkladatele
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http://linked.open...dnocenehoVysledku
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http://linked.open...ai/riv/idVysledku
| - RIV/00209805:_____/10:#0000115
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http://linked.open...riv/jazykVysledku
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http://linked.open.../riv/klicovaSlova
| - LA-12, cisplatin, Hsp90 (en)
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http://linked.open.../riv/klicoveSlovo
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http://linked.open...odStatuVydavatele
| - GB - Spojené království Velké Británie a Severního Irska
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http://linked.open...ontrolniKodProRIV
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http://linked.open...i/riv/nazevZdroje
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http://linked.open...in/vavai/riv/obor
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http://linked.open...ichTvurcuVysledku
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http://linked.open...cetTvurcuVysledku
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http://linked.open...vavai/riv/projekt
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http://linked.open...UplatneniVysledku
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http://linked.open...v/svazekPeriodika
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http://linked.open...iv/tvurceVysledku
| - Hrstka, Roman
- Kvardová, Veronika
- Vojtěšek, Bořivoj
- Müller, Petr
- Matoulková, Eva
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http://linked.open...ain/vavai/riv/wos
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http://linked.open...n/vavai/riv/zamer
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issn
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number of pages
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