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Statements

Subject Item
n2:RIV%2F61989592%3A15310%2F04%3A00002152%21RIV%2F2005%2FMSM%2F153105%2FN
rdf:type
n15:Vysledek skos:Concept
dcterms:description
Altered phosphorylation of cellular proteins stimulated an extensive search for protein kinase inhibitors as drugs. Cyclin-dependent kinases (CDKs), enzymes involved in diverse cellular processes, including cell division cycle, transcription, differentiation and apoptosis, are suitable targets of such inhibitors with potential application in cancer therapy1. One of the first reported specific CDK inhibitors, olomoucine, had became a leading compound of the development based on structure-activity relatioships, that led to the synthesis of roscovitine2 and olomoucine II (ref.3), respectively. Both derivatives show an enhanced CDK inhibitory activity, increased selectivity and antiproliferative activity. Moreover, roscovitine has been also shown to induce nuclear accumulation of tumour suppressor p53 and enhance p53-dependent transcription in human cancer cells4. The novel derivative olomoucine II inhibits CDKs more efficiently and causes cell cycle blocks at G1/S and G2/M transitions stronger than rosc Změněná fosforylace buněčných proteinů v nádorových buňkách vyvolala zájem o inhibitory proteinkinas jako potenciální léčiva. Cyklin-dependentní kinasy (CDK), které řídí různé buněčné procesy od buněčného cyklu, přes transkripci, diferenciaci a apoptózu, patří ovněž mezi farmakologické zajímavé cíle. Jeden z prvních specifických inhibitorů CDK olomoucin se stal výchozím bodem pro vývoj účinnějších inhibitorů, např. roskovitinu anebo olomoucinu II. Obě tyto látky již vykazují vysokou účinnost a specifitu. Roskovitin navíc indukuje akumulaci nádorového supresoru p53 v jádře a podporuje jeho transkripční aktivitu. Nový inhibitor olomoucin II pak patří k jeětě účinnějším inhibitorům buněčné proliferace. Naše výsledky potvrují, že antiproliferační aktivita inhibitorů CDK je způsobena přímou inhibicí CDK a indukcí p53, což vyzdvihuje možné farmakologické aplikace inhibitorů CDK. Altered phosphorylation of cellular proteins stimulated an extensive search for protein kinase inhibitors as drugs. Cyclin-dependent kinases (CDKs), enzymes involved in diverse cellular processes, including cell division cycle, transcription, differentiation and apoptosis, are suitable targets of such inhibitors with potential application in cancer therapy1. One of the first reported specific CDK inhibitors, olomoucine, had became a leading compound of the development based on structure-activity relatioships, that led to the synthesis of roscovitine2 and olomoucine II (ref.3), respectively. Both derivatives show an enhanced CDK inhibitory activity, increased selectivity and antiproliferative activity. Moreover, roscovitine has been also shown to induce nuclear accumulation of tumour suppressor p53 and enhance p53-dependent transcription in human cancer cells4. The novel derivative olomoucine II inhibits CDKs more efficiently and causes cell cycle blocks at G1/S and G2/M transitions stronger than rosc
dcterms:title
Antiproliferative activity of Olomoucine II, a novel cyclin-dependent kinase inhibitor Antiproliferative activity of Olomoucine II, a novel cyclin-dependent kinase inhibitor Antiproliferativní účinky nového inhibitoru CDK, olomoucinu II
skos:prefLabel
Antiproliferativní účinky nového inhibitoru CDK, olomoucinu II Antiproliferative activity of Olomoucine II, a novel cyclin-dependent kinase inhibitor Antiproliferative activity of Olomoucine II, a novel cyclin-dependent kinase inhibitor
skos:notation
RIV/61989592:15310/04:00002152!RIV/2005/MSM/153105/N
n3:strany
133
n3:aktivita
n16:Z
n3:aktivity
Z(MSM 153100008)
n3:cisloPeriodika
Suppl.
n3:dodaniDat
n5:2005
n3:domaciTvurceVysledku
n6:9961216 n6:3151948 n6:9637419 n6:4712048
n3:druhVysledku
n14:J
n3:duvernostUdaju
n17:S
n3:entitaPredkladatele
n10:predkladatel
n3:idSjednocenehoVysledku
554842
n3:idVysledku
RIV/61989592:15310/04:00002152
n3:jazykVysledku
n12:eng
n3:klicovaSlova
CDK;inhibitor;p53;anticancer drug
n3:klicoveSlovo
n8:CDK n8:p53 n8:anticancer%20drug n8:inhibitor
n3:kodStatuVydavatele
CZ - Česká republika
n3:kontrolniKodProRIV
[FED9727C0065]
n3:nazevZdroje
Acta Universitatis Palackianae Olomucensis, Facultas Rerum Naturalium, Chemica
n3:obor
n13:ED
n3:pocetDomacichTvurcuVysledku
4
n3:pocetTvurcuVysledku
5
n3:rokUplatneniVysledku
n5:2004
n3:svazekPeriodika
43
n3:tvurceVysledku
Otyepka, Michal Orság, Martin Vojtěšek, Bořivoj Strnad, Miroslav Kryštof, Vladimír
n3:zamer
n18:MSM%20153100008
s:issn
0232-0061
s:numberOfPages
278
n11:organizacniJednotka
15310