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| rdf:type
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| Description
| - 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. (cs)
- 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
- 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 (en)
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| Title
| - Antiproliferative activity of Olomoucine II, a novel cyclin-dependent kinase inhibitor
- Antiproliferative activity of Olomoucine II, a novel cyclin-dependent kinase inhibitor (en)
- Antiproliferativní účinky nového inhibitoru CDK, olomoucinu II (cs)
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| skos:prefLabel
| - Antiproliferative activity of Olomoucine II, a novel cyclin-dependent kinase inhibitor
- Antiproliferative activity of Olomoucine II, a novel cyclin-dependent kinase inhibitor (en)
- Antiproliferativní účinky nového inhibitoru CDK, olomoucinu II (cs)
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| skos:notation
| - RIV/61989592:15310/04:00002152!RIV/2005/MSM/153105/N
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| http://linked.open.../vavai/riv/strany
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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/61989592:15310/04:00002152
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| http://linked.open...riv/jazykVysledku
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| http://linked.open.../riv/klicovaSlova
| - CDK;inhibitor;p53;anticancer drug (en)
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| http://linked.open.../riv/klicoveSlovo
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| http://linked.open...odStatuVydavatele
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| http://linked.open...ontrolniKodProRIV
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| http://linked.open...i/riv/nazevZdroje
| - Acta Universitatis Palackianae Olomucensis, Facultas Rerum Naturalium, Chemica
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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...UplatneniVysledku
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| http://linked.open...v/svazekPeriodika
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| http://linked.open...iv/tvurceVysledku
| - Kryštof, Vladimír
- Otyepka, Michal
- Strnad, Miroslav
- Vojtěšek, Bořivoj
- Orság, Martin
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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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| http://localhost/t...ganizacniJednotka
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