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The selective P-TEFb inhibitor CAN508 targets angiogenesise
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SYSNO ASEP 0368596 Document Type J - Journal Article R&D Document Type Journal Article Subsidiary J Článek ve WOS Title The selective P-TEFb inhibitor CAN508 targets angiogenesise Author(s) Kryštof, Vladimír (UEB-Q) RID, ORCID
Rárová, Lucie (UEB-Q) RID, ORCID
Liebl, J. (DE)
Zahler, S. (DE)
Jorda, Radek (UEB-Q) ORCID, RID
Voller, Jiří (UEB-Q) RID, ORCID
Cankař, Petr (UEB-Q) ORCIDNumber of authors 7 Source Title European Journal of Medicinal Chemistry. - : Elsevier - ISSN 0223-5234
Roč. 46, č. 9 (2011), s. 4289-4294Number of pages 6 s. Language eng - English Country FR - France Keywords Angiogenesis ; Cancer ; Transcription ; Inhibitor ; Cyclin-dependent kinase 9 Subject RIV CE - Biochemistry R&D Projects GA204/08/0511 GA ČR - Czech Science Foundation (CSF) GA301/08/1649 GA ČR - Czech Science Foundation (CSF) CEZ AV0Z50380511 - UEB-Q (2005-2011) UT WOS 000295237400081 DOI 10.1016/j.ejmech.2011.06.035 Annotation 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. Workplace Institute of Experimental Botany Contact David Klier, knihovna@ueb.cas.cz, Tel.: 220 390 469 Year of Publishing 2012
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