Počet záznamů: 1
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 Druh ASEP J - Článek v odborném periodiku Zařazení RIV J - Článek v odborném periodiku Poddruh J Článek ve WOS Název A Novel Roscovitine Derivative Potently Induces G(1)-Phase Arrest in Platelet-Derived Growth Factor-BB-Activated Vascular Smooth Muscle Cells Tvůrce(i) 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)Zdroj.dok. Molecular Pharmacology - ISSN 0026-895X
Roč. 77, č. 2 (2010), s. 255-261Poč.str. 7 s. Jazyk dok. eng - angličtina Země vyd. US - Spojené státy americké Klíč. slova CYCLIN-DEPENDENT KINASES ; DRUG-ELUTING STENTS ; CYC202 R-ROSCOVITINE Vědní obor RIV FD - Onkologie a hematologie CEP GA301/08/1649 GA ČR - Grantová agentura ČR CEZ AV0Z50380511 - UEB-Q (2005-2011) UT WOS 000273725600016 DOI 10.1124/mol.109.060327 Anotace 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. Pracoviště Ústav experimentální botaniky Kontakt David Klier, knihovna@ueb.cas.cz, Tel.: 220 390 469 Rok sběru 2011
Počet záznamů: 1