. . . . . " inhibitors" . . "2005-01-01+01:00"^^ . "Aim of this grant is to develop new generations of inhibitors of cyclin-dependent kinases (CDK). We (1) prepared new OC-type inhibitors - olomoucine II, (2) studied their structure-activity relationship in different kinase assays, (3)developed new genera"@en . " cyclin-dependent kinases" . . "2007-12-31+01:00"^^ . . . . "New generations of cyclin-dependent kinase inhibitors with significant anticancer properties"@en . . . "1"^^ . "cell cycle" . . . "2"^^ . "2007-05-02+02:00"^^ . . . . "Characterization of cytokinin derivative olomoucine (OC; 2-(2-hydroxyethylamino)-6-benzylamino-9-methylpurine) as one of the first specific inhibitors of cyclin-dependent kinases (cdc2, cdk2, cdk5) has shown the possibility to inhibit important phases ofcell cycle such as G1/S and G2/M transition. The design and inhibitory activity of OC was further improved by modifications at positions 2,6 and 9. This has recently led to discovery of bohemine, roscovitine, purvalanol A, and olomoucine II, which display an enhanced inhibitory activity toward CDK1, increased antimitotic activity at the G1/S and G2/M transitions of the cell division cycle, and stronger and more potent antitumour effects. In this project we would like: (1) to prepare new OC-type inhibitors, (2) to develop new generations of CDK inhibitors structurally unrelated to trisubstituted purines like pyrazolo[ 4,3-d] pyrimidines and triazoles, (3) to study their structure-activity relationship in different kinase assays, (4) to use"@en . "0"^^ . "2008-12-16+01:00"^^ . . "Charakterizace cytokininov\u00E9ho deriv\u00E1tu olomoucinu (OC, 2-(2-hydroxyethylamino)-6-benzylamino-9-methylpurin) jako jednoho z prvn\u00EDch specifick\u00FDch inhibitor\u016F cyklin-dependentn\u00ED kinas (cdk1, cdk2, cdk5) uk\u00E1zala na mo\u017Enost inhibice d\u016Fle\u017Eit\u00FDch f\u00E1z\u00ED bun\u011B\u010Dn\u00E9ho cyklu (p\u0159echody G1/S a G2/M). Toto zji\u0161t\u011Bn\u00ED logicky p\u0159ineslo v\u00FDvoj i nov\u00E9 generace protin\u00E1dorov\u00FDch l\u00E1tek na antimitotick\u00E9m z\u00E1klad\u011B, nap\u0159. boheminu, roskovitinu, olomoucinu II a purvalanolu A. Na\u0161\u00EDm c\u00EDlem je pokra\u010Dovat ve v\u00FDvoji dal\u0161\u00EDch, je\u0161t\u011B \u00FA\u010Dinn\u011Bj\u0161\u00EDchinhibitor\u016F CDK, kter\u00FD bude zahrnovat: (1) p\u0159\u00EDpravu nov\u00FDch typ\u016F inhibitor\u016F CDK odvozen\u00FDch od OC, (2) v\u00FDvoj nov\u00FDch generac\u00ED inhibitor\u016F CDK na b\u00E1zi pyrazolo[ 4,3-d] pyrimidin\u016F and triazol\u016F, (3) studium vztah\u016F mezi strukturou a aktivitou v r\u016Fzn\u00FDch kinasov\u00FDchtestech, (4) vyu\u017Eit\u00ED proteomiky k anal\u00FDze \u00FA\u010Dink\u016F t\u011Bchto l\u00E1tek na bun\u011B\u010Dn\u00E9 \u00FArovni, (5) testov\u00E1n\u00ED na \u00FA\u010Dinky cytotoxick\u00E9, apoptoick\u00E9 a na bun\u011B\u010Dn\u00FD cyklus u \u017Eivo\u010Di\u0161n\u00FDch i rostlinn\u00FDch bun\u011Bk, (6) hled\u00E1n\u00ED nov\u00FDch molekul\u00E1rn\u00EDch c\u00EDl\u016F v n\u00E1dorov\u00E9 bu\u0148ce pomoc\u00ED afinitn\u00ED" . "Nov\u00E9 generace inhibitor\u016F cyklin-dependentn\u00EDch kinas s v\u00FDznamn\u00FDmi protin\u00E1dorov\u00FDmi \u00FA\u010Dinky" . . "Pokra\u010Dovali jsme ve v\u00FDvoji dal\u0161\u00EDch, je\u0161t\u011B \u00FA\u010Dinn\u011Bj\u0161\u00EDch inhibitor\u016F CDK: (1) p\u0159ipravili jsme nov\u00E9 typy inhibitor\u016F CDK, nap\u0159 olomoucin II, (2) studovali jsme vztahy mezi strukturou a aktivitou v r\u016Fzn\u00FDch kinasov\u00FDch testech, (3) vyvinuli jsme nov\u00E9 generace inh"@cs . "http://www.isvav.cz/projectDetail.do?rowId=GA301/05/0418"^^ . "GA301/05/0418" . . "10"^^ . "cell cycle; cyclin-dependent kinases; inhibitors; cancer"@en . "10"^^ .