Počet záznamů: 1

The selective P-TEFb inhibitor CAN508 targets angiogenesise

  1. 1.
    0368596 - UEB-Q 2012 RIV FR eng J - Článek v odborném periodiku
    Kryštof, Vladimír - Rárová, Lucie - Liebl, J. - Zahler, S. - Jorda, Radek - Voller, Jiří - Cankař, Petr
    The selective P-TEFb inhibitor CAN508 targets angiogenesise.
    European Journal of Medicinal Chemistry. Roč. 46, č. 9 (2011), s. 4289-4294 ISSN 0223-5234
    Grant CEP: GA ČR GA204/08/0511; GA ČR GA301/08/1649
    Výzkumný záměr: CEZ:AV0Z50380511
    Klíčová slova: Angiogenesis * Cancer * Transcription * Inhibitor * Cyclin-dependent kinase 9
    Kód oboru RIV: CE - Biochemie
    Impakt faktor: 3.346, rok: 2011

    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.
    Trvalý link: http://hdl.handle.net/11104/0202895