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A Novel Roscovitine Derivative Potently Induces G(1)-Phase Arrest in Platelet-Derived Growth Factor-BB-Activated Vascular Smooth Muscle Cells
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SYSNO ASEP 0344007 Document Type J - Journal Article R&D Document Type Journal Article Subsidiary J Článek ve WOS Title A Novel Roscovitine Derivative Potently Induces G(1)-Phase Arrest in Platelet-Derived Growth Factor-BB-Activated Vascular Smooth Muscle Cells Author(s) Sroka, I. M. (AT)
Heiss, E.H. (AT)
Havlíček, Libor (UEB-Q) RID, ORCID
Totzke, F. (DE)
Aristei, Y. (IT)
Pechan, P. (DE)
Kubbutat, M.H.G. (DE)
Strnad, Miroslav (UEB-Q) RID, ORCID
Dirsch, V.M. (AT)Source Title Molecular Pharmacology - ISSN 0026-895X
Roč. 77, č. 2 (2010), s. 255-261Number of pages 7 s. Language eng - English Country US - United States Keywords CYCLIN-DEPENDENT KINASES ; DRUG-ELUTING STENTS ; CYC202 R-ROSCOVITINE Subject RIV FD - Oncology ; Hematology R&D Projects GA301/08/1649 GA ČR - Czech Science Foundation (CSF) CEZ AV0Z50380511 - UEB-Q (2005-2011) UT WOS 000273725600016 DOI 10.1124/mol.109.060327 Annotation Abnormal vascular smooth muscle cell (VSMC) proliferation contributes to the pathogenesis of restenosis. Thus, drugs interfering with cell cycle progression in VSMC are promising candidates for an antirestenotic therapy. In this study, we pharmacologically characterize N-5-(2-aminocyclohexyl)-N-7-benzyl-3-isopropyl-1(2)H-pyrazolo[4,3-d]pyrimidine-5,7-di-amine (LGR1406), a novel derivative of the cyclin-dependent kinase (CDK) inhibitor roscovitine (ROSC), in PDGF-BB-activated VSMC. Cell proliferation was quantified measuring DNA synthesis via 5-bromo-2'-deoxyuridine incorporation. Analysis of cell cycle distribution was done by flow cytometry using propidium iodide-stained nuclei. Key regulators of the cell cycle and relevant signaling pathways were dissected by Western blot analyses. In addition, in vitro kinase assays and in silico studies regarding the pharmacokinetic profile of both compounds were performed. Workplace Institute of Experimental Botany Contact David Klier, knihovna@ueb.cas.cz, Tel.: 220 390 469 Year of Publishing 2011
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