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Statements

Subject Item
n2:RIV%2F00209805%3A_____%2F10%3A%230000115%21RIV11-MZ0-00209805
rdf:type
n12:Vysledek skos:Concept
dcterms: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.
dcterms: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
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
skos:notation
RIV/00209805:_____/10:#0000115!RIV11-MZ0-00209805
n3:aktivita
n17:Z n17:P
n3:aktivity
P(NS9812), Z(MZ0MOU2005)
n3:cisloPeriodika
15.6.2010
n3:dodaniDat
n5:2011
n3:domaciTvurceVysledku
n13:5395488 n13:1895214 n13:1330586 n13:9637419 n13:7675011
n3:druhVysledku
n6:J
n3:duvernostUdaju
n16:S
n3:entitaPredkladatele
n14:predkladatel
n3:idSjednocenehoVysledku
274738
n3:idVysledku
RIV/00209805:_____/10:#0000115
n3:jazykVysledku
n11:eng
n3:klicovaSlova
LA-12, cisplatin, Hsp90
n3:klicoveSlovo
n4:Hsp90 n4:cisplatin n4:LA-12
n3:kodStatuVydavatele
GB - Spojené království Velké Británie a Severního Irska
n3:kontrolniKodProRIV
[4C5D7D1A9DEC]
n3:nazevZdroje
Molecular cancer
n3:obor
n18:FD
n3:pocetDomacichTvurcuVysledku
5
n3:pocetTvurcuVysledku
9
n3:projekt
n15:NS9812
n3:rokUplatneniVysledku
n5:2010
n3:svazekPeriodika
9
n3:tvurceVysledku
Vojtěšek, Bořivoj Kvardová, Veronika Hrstka, Roman Müller, Petr Matoulková, Eva
n3:wos
000279281100001
n3:zamer
n7:MZ0MOU2005
s:issn
1476-4598
s:numberOfPages
9