About: The selective P-TEFb inhibitor CAN508 targets angiogenesise

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An Entity of Type : http://linked.opendata.cz/ontology/domain/vavai/Vysledek, within Data Space : linked.opendata.cz associated with source document(s)

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rdf:type	skos:Concept http://linked.opendata.cz/ontology/domain/vavai/Vysledek
Description	Small molecule inhibitors of cyclin-dependent kinases (CDK) have been developed as anticancer drugs with cytostatic and cytotoxic properties, but some of them have also been shown to limit angiogenesis. Here, we report that the 3,5-diaminopyrazole CAN508 inhibits endothelial cell migration and tube formation. In addition, it reduces phosphorylation of the C-terminus of RNA polymerase II and inhibits mRNA synthesis in endothelial cells, in accordance with previous observations that it has high selectivity towards the positive transcriptional regulator P-TEFb. Moreover, CAN508 reduces expression of vascular endothelial growth factor by several human cancer cell lines. The findings suggest that P-TEFb may be an attractive target for anti-angiogenic therapy. (C) 2011 Elsevier Masson SAS. All rights reserved. Small molecule inhibitors of cyclin-dependent kinases (CDK) have been developed as anticancer drugs with cytostatic and cytotoxic properties, but some of them have also been shown to limit angiogenesis. Here, we report that the 3,5-diaminopyrazole CAN508 inhibits endothelial cell migration and tube formation. In addition, it reduces phosphorylation of the C-terminus of RNA polymerase II and inhibits mRNA synthesis in endothelial cells, in accordance with previous observations that it has high selectivity towards the positive transcriptional regulator P-TEFb. Moreover, CAN508 reduces expression of vascular endothelial growth factor by several human cancer cell lines. The findings suggest that P-TEFb may be an attractive target for anti-angiogenic therapy. (C) 2011 Elsevier Masson SAS. All rights reserved. (en)
Title	The selective P-TEFb inhibitor CAN508 targets angiogenesise The selective P-TEFb inhibitor CAN508 targets angiogenesise (en)
skos:prefLabel	The selective P-TEFb inhibitor CAN508 targets angiogenesise The selective P-TEFb inhibitor CAN508 targets angiogenesise (en)
skos:notation	RIV/61389030:_____/11:00368596!RIV12-AV0-61389030
http://linked.open...avai/riv/aktivita	P Z
http://linked.open...avai/riv/aktivity	P(ED0007/01/01), P(GA204/08/0511), P(GA301/08/1649), Z(AV0Z50380511), Z(MSM6198959216)
http://linked.open...iv/cisloPeriodika	9
http://linked.open...vai/riv/dodaniDat	2012
http://linked.open...aciTvurceVysledku	Jorda, Radek Voller, Jiří Kryštof, Vladimír Rárová, Lucie Cankař, Petr
http://linked.open.../riv/druhVysledku	J - Článek v odborném periodiku
http://linked.open...iv/duvernostUdaju	S - Úplné a pravdivé údaje nepodléhající ochraně podle zvláštních právních předpisů
http://linked.open...titaPredkladatele	Ústav experimentální botaniky AV ČR, v. v. i.
http://linked.open...dnocenehoVysledku	228697
http://linked.open...ai/riv/idVysledku	RIV/61389030:_____/11:00368596
http://linked.open...riv/jazykVysledku	eng - angličtina
http://linked.open.../riv/klicovaSlova	Angiogenesis; Cancer; Transcription; Inhibitor; Cyclin-dependent kinase 9 (en)
http://linked.open.../riv/klicoveSlovo	Angiogenesis Cancer Inhibitor Cyclin-dependent kinase 9 Transcription
http://linked.open...odStatuVydavatele	FR - Francouzská republika
http://linked.open...ontrolniKodProRIV	[C7C8009FACBA]
http://linked.open...i/riv/nazevZdroje	European Journal of Medicinal Chemistry
http://linked.open...in/vavai/riv/obor	CE
http://linked.open...ichTvurcuVysledku	5 (xsd:int)
http://linked.open...cetTvurcuVysledku	7 (xsd:int)
http://linked.open...vavai/riv/projekt	Biological activity of synthetic inhibitors of cyclin-dependent kinases Centre of the Region Haná for Biotechnological and Agricultural Research Modulation of cell division of normal and cancer cells by cyclin-dependent kinase inhibitors
http://linked.open...UplatneniVysledku	2011
http://linked.open...v/svazekPeriodika	46
http://linked.open...iv/tvurceVysledku	Jorda, Radek Kryštof, Vladimír Liebl, J. Voller, Jiří Zahler, S. Cankař, Petr Rárová, Lucie
http://linked.open...ain/vavai/riv/wos	000295237400081
http://linked.open...n/vavai/riv/zamer	Mechanismy regulace růstu a vývoje rostlin na úrovni buněk, orgánů a celých organismů: fyziologické, genetické a molekulárně biologické základy Modulation of signalling and regulatory pathways in normal and cancer cells
issn	0223-5234
number of pages	6 (xsd:int)
http://bibframe.org/vocab/doi	10.1016/j.ejmech.2011.06.035

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