Olomoucin II, nový inhibitor cyklin-dependentní kinasy, indukuje silnou transktipci p53

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61989592%3A15310%2F04%3A00002153" target="_blank" >RIV/61989592:15310/04:00002153 - isvavai.cz</a>

Výsledek na webu

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DOI - Digital Object Identifier

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Jazyk výsledku

angličtina

Název v původním jazyce

Olomoucine II, a novel cyclin-dependent kinase inhibitor, induces strong p53-dependent transcription

Popis výsledku v původním jazyce

Cyclin-dependent kinases (CDKs), enzymes involved in diverse cellular processes, including cell division cycle, transcription, differentiation and apoptosis, are suitable targets of inhibitors with potential application in cancer therapy. One of the first reported specific CDK inhibitors, olomoucine, had became a leading compound of the research, that led to development of roscovitine and olomoucine II, respectively. Both derivatives show an enhanced CDK inhibitory activity, increased selectivity and antiproliferative activity. The novel derivative olomoucine II inhibits some CDKs more efficiently (CDK1/2/4/7), causes cell cycle blocks at G1/S and G2/M transitions and exhibits stronger and more selective antitumor effects. Moreover, olomoucine II induces nuclear accumulation of tumor suppressor p53 at low micromolar level. An enhancement of p53-dependent transcription in human cancer cells also coincides with p21WAF1 induction. The results demonstrate that the antiproliferative activit

Název v anglickém jazyce

Olomoucine II, a novel cyclin-dependent kinase inhibitor, induces strong p53-dependent transcription

Popis výsledku anglicky

Cyclin-dependent kinases (CDKs), enzymes involved in diverse cellular processes, including cell division cycle, transcription, differentiation and apoptosis, are suitable targets of inhibitors with potential application in cancer therapy. One of the first reported specific CDK inhibitors, olomoucine, had became a leading compound of the research, that led to development of roscovitine and olomoucine II, respectively. Both derivatives show an enhanced CDK inhibitory activity, increased selectivity and antiproliferative activity. The novel derivative olomoucine II inhibits some CDKs more efficiently (CDK1/2/4/7), causes cell cycle blocks at G1/S and G2/M transitions and exhibits stronger and more selective antitumor effects. Moreover, olomoucine II induces nuclear accumulation of tumor suppressor p53 at low micromolar level. An enhancement of p53-dependent transcription in human cancer cells also coincides with p21WAF1 induction. The results demonstrate that the antiproliferative activit

Druh

D - Stať ve sborníku

CEP obor

ED - Fyziologie

OECD FORD obor

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Projekt

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Návaznosti

Z - Vyzkumny zamer (s odkazem do CEZ)

Rok uplatnění

2004

Kód důvěrnosti údajů

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Název statě ve sborníku

Cell Cycle and Cancer: Pathways and Therapies

ISBN

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ISSN

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e-ISSN

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Počet stran výsledku

225

Strana od-do

"A3"

Název nakladatele

American Association for Cancer Research

Místo vydání

Florida

Místo konání akce

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Datum konání akce

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Typ akce podle státní příslušnosti

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Kód UT WoS článku

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