Anti-angiogenic effects of purine inhibitors of cyclin dependent kinases

0368597 - ÚEB 2012 RIV NL eng J - Journal Article
Liebl, J. - Kryštof, Vladimír - Vereb, G. - Takacs, L. - Strnad, Miroslav - Pechan, P. - Havlíček, Libor - Zatloukal, Marek - Fuerst, R. - Vollmar, A. M. - Zahler, S.
Anti-angiogenic effects of purine inhibitors of cyclin dependent kinases.
Angiogenesis. Roč. 14, č. 3 (2011), s. 281-291. ISSN 0969-6970. E-ISSN 1573-7209
R&D Projects: GA ČR GA204/08/0511; GA ČR GA301/08/1649
Institutional research plan: CEZ:AV0Z50380511
Keywords : Angiogenesis * Cdk * Small molecule Cdk inhibitors * Roscovitine
Subject RIV: CE - Biochemistry
Impact factor: 6.063, year: 2011

Small molecular inhibitors of Cyclin dependent kinases (Cdks) are currently being developed as anticancer therapeutics due to their antiproliferative properties. The purine Cdk specific inhibitor (R)-roscovitine (seliciclib, CYC202) represents one of the most promising of these compounds. It is currently evaluated in clinical trials concerning cancer therapy. Recently, we have shown that roscovitine exerts potent antiangiogenic effects and elucidated Cdk5 as a new player in angiogenesis. These findings introduce Cdk5 as novel target for antiangiogenic therapy, and Cdk5 inhibitors as an attractive therapeutic approach. Here, we present the antiangiogenic profile of 15 derivatives of roscovitine in vitro and in vivo and provide structure activity relationships of the roscovitine analogs.
Permanent Link: http://hdl.handle.net/11104/0202896