Cyclin-dependent kinases inhibitor
S-Like-Phase Cyclin-Dependent Kinases Stabilize the Epstein-Barr Virus BDLF4 Protein To Temporally Control Late Gene Transcription
... FIG 3 CDK inhibitors suppress BDLF4 phosphorylation, destabilizing the protein. (A) (Left) HEK293 cells were transfected with a BDLF4 expression plasmid together with an EGFP expression plasmid (as a control) and were ...
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Transactivation of Herpes Simplex Virus Type 1 Immediate-Early Gene Expression by Virion-Associated Factors Is Blocked by an Inhibitor of Cyclin-Dependent Protein Kinases
... There are several possible sites at which Roscovitine may act, and they are described in the following discussions: (i) In vitro studies have characterized the molecular mechanism of VP16-dependent transcriptional ...
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Transcription of Herpes Simplex Virus Immediate-Early and Early Genes Is Inhibited by Roscovitine, an Inhibitor Specific for Cellular Cyclin-Dependent Kinases
... Involvement of cdks in viral functions. Cellular cdks have long been known to be involved in the replication of DNA- containing viruses (21, 23, 60). For example, the replication of simian virus 40 and polyomavirus DNAs ...
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A Chrysin Derivative Suppresses Skin Cancer Growth by Inhibiting Cyclin-dependent Kinases
... these kinases have long been considered ideal targets for anti- cancer ...for cyclin A association (26). A phytochemical Cdk inhibitor described as an ATP-noncompetitive inhibitor has also ...
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Synthesis of ring constrained thiazolylpyrimidines: inhibitors of cyclin dependent kinases
... With regard to cellular antiproliferative potency, compound 9g, the prototype compound from the 2-anilino-4-(thiazol-5-yl)pyrimidine family, was found to possess lower activity against human tumour cell lines than might ...
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Omega 3 polyunsaturated fatty acids inhibit cell proliferation by regulating cell cycle in fad3b transgenic mouse embryonic stem cells
... G1/S-specific cyclin-D1; Ccne1: G1/S-specific cyclin-E1; Cdk2: Cyclin- dependent kinase 2; Cdk4: Cyclin-dependent kinase 4; Cdk6: Cyclin-dependent kinase 6; Cdkn1a: ...
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Anti cancer activity of Psoralea fructus through the downregulation of cyclin D1 and CDK4 in human colorectal cancer cells
... upstream kinases associated with PF-mediated degradation of cyclin D1 and CDK4 pro- tein, HCT116 cells were pretreated with PD98059 (20 μ M, inhibitor of extracellular signal – regulated kinase 1/2 ...
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Cyclin-Dependent Kinase Inhibitor AT7519 as a Potential Drug for MYCN-Dependent Neuroblastoma.
... CDK inhibitor AT7519 in neuroblastoma ...CDK2 inhibitor that binds within the active site cleft of CDK2 overlapping with the ATP-binding pocket (13), it also effectively targets additional kinases ...
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Roscovitine, a Specific Inhibitor of Cellular Cyclin-Dependent Kinases, Inhibits Herpes Simplex Virus DNA Synthesis in the Presence of Viral Early Proteins
... fident that the inhibition observed in these experiments is an underestimate of the actual inhibitory effect of Rosco on viral DNA synthesis. Third, the three known or putative viral ki- nases are all nonessential in ...
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Kaposi's Sarcoma-Associated Herpesvirus K-bZIP Protein Is Phosphorylated by Cyclin-Dependent Kinases
... Antibodies. An anti-K-bZIP rabbit serum was raised against the protein prod- uct of pRSET-K-bZIPSE by Animal Farm Services (Healdsberg, Calif.). To produce K-bZIPSE BL21(DE3)-pLysS, cells were transformed with pRSET-K- ...
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Investigation of the role of cyclin dependent kinases in neuronal apoptosis
... The Cip/Kip family of CKIs is characterised by their binding to preformed Cdk/cyclin complexes (Harper et aL, 1993; Polyak et aL, 1994; Lee et aL, 1995) (Figure 1.2). In vitro, these CKIs can block the activity of ...
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Inhibitors of cyclin-dependent kinases as cancer therapeutics.
... which are either approved or in advanced registration trials for several cancers. The discovery and clinical development of these drugs, and in particular, the FDA approval for palbociclib in ER+ breast cancer, has ...
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Transforming growth factor β and breast cancer: Cell cycle arrest by transforming growth factor β and its disruption in cancer
... Cdc25A, cyclin E and cyclin A genes, and an increase in the association of p15, p21 and p27 with target ...1 cyclin–cdks leads to pRb dephosphorylation and E2F ...of cyclin–cdk regula- tion in ...
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The PHOA and PHOB Cyclin-Dependent Kinases Perform an Essential Function in Aspergillus nidulans
... PHOA cyclin-dependent kinase (CDK) of Aspergillus nidulans plays no role in regulation of enzymes involved in phosphorous acquisition but instead modulates differentiation in response to environmental ...
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The effect of cyclic adenosine monophosphate (camp) modulators on the activity of selected antimalarial drugs
... the ste6 gene of saccharomyces cerevisiae with pfmdr1 gene of Plasmodium falciparum. and Geyer, J.A. Cyclin-dependent protein kinases as therapeutic drug targets for antimalarial drug de[r] ...
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Indirect p53-dependent transcriptional repression of Survivin CDC25C , and PLK1 genes requires the cyclin-dependent kinase inhibitor p21/CDKN1A and CDE/CHR promoter sites binding the DREAM complex
... When looking at p53 association with DNA by ChIP, no significant binding of p53 was observed to the promoters of Survivin, CDC25C, and PLK1, in contrast to the promoters of cyclin-dependent kinase (CDK) ...
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Requirement for Cellular Cyclin-Dependent Kinases in Herpes Simplex Virus Replication and Transcription
... cellular kinases (other than cdks) and inhibitors of cell cycle progression that do not block cdks do not block viral replication, and (v) a structural isomer of Olo that does not inhibit cdk activity does not ...
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Cyclin dependent kinase inhibitor 2B regulates efferocytosis and atherosclerosis
... are dysregulated in carriers of the 9p21 risk variant. Though a variety of associations have been reported (8–12), reduced expres- sion of the nearby tumor-suppressor gene CDKN2B has now been observed in several tissues ...
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Transformation of SV40-immortalized human uroepithelial cells by 3-methylcholanthrene increases IFN- and Large T Antigen-induced transcripts
... Clearly the IFN-g pathways activated by 3-MC were not intrinsically growth-suppressive in nature, since HUC-TC exhibited more rapid growth than HUC in the absence of treatment with exogenous IFN-g. Activation of IFN-g- ...
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Pharmacokinetics and biodistribution of the cyclin-dependent kinase inhibitor -CR8- in mice
... Recently, the tri-substituted purine CR8 was introduced as a selective second generation CDK inhibitor analogue of roscovitine [6,7]. In-vitro studies have shown that CR8 is 2–4 fold more potent as a CDK ...
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