Global ETD Search
Search theses and dissertations gathered from participating repositories worldwide. Every result links back to the library that holds it. No account is needed.
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Showing 1 to 20 of 23 for “"CDK inhibitors"”.
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Design of Non-ATP Competitive and Cell Cycle Specific CDK Inhibitors Targeting Cyclin Binding Groove
<p>CDK2/cyclin A and CDK4/cyclin D1 are validated targets for cancer drug discovery with ATP competitive compounds being the most common inhibitors. However, issues arising from the selectivity of current inhibitors have prevented clinical validation of these important targets. To generate cell …
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The Effect of Endothelin-1 on the expression of CDK Inhibitors p21 & p27 in Bovine Corneal Endothelial Cells
… the down regulation of cyclin dependant kinase inhibitors (p21cip1 and p27kip1) levels by Endothelin-1 (ET-1), would overcome the G1 phase arrest and promote cell cycle progression and proliferation in cultured BCECs (Bovine corneal endothelial cells). BCECs were isolated from bovine corneas and …
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Targeting CDK to Prevent and Treat Retinoblastoma and other Cancers
Pharmaceutical investment in cell cycle inhibitors has been immense, yet the efficacy in treating established tumors is poor in most cases. Considering that tumor cells co-opt the cell cycle to grow, it is unclear why most cell cycle inhibitors, like CDK inhibitors, have failed to pass Phase II …
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Isolation and characterization of the SIAMESE family: a novel class of cell cycle regulators in plants
… found in the Kip-related (KRP) class of plant CDK inhibitors, and a "Cy" motif found in CDK inhibitors, E2F and Retinoblastoma in animals. Accordingly, SIM was found to associate with D-type cyclins as well as CDKA;1 in vivo. Although no interactions were detected between SIM and mitotic B-type …
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Design and Synthesis of Novel Benzimidazoles and Aminothiazoles as Small Molecule Inhibitors of CDK5/p25
… synthesis and biological evaluation of novel CDK5/p25 small molecule inhibitors. Cyclin dependent kinase 5 (CDK5) is a proline directed serine/threonine kinase which plays an important role in the pathology of Alzheimer's disease (AD). CDK5/p25 has been implicated in hyperphosphorylation of …
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Increasing IFN-[gamma] productivity in CHO cells through CDK inhibition
… of siRNA and chemical cyclin dependent kinase (CDK) inhibitors, we have developed new methods to improve and better understand recombinant protein production during growth arrest. In this study, we have shown that the specific inhibition of the CDK2-CcnE complex through chemical inhibition leads …
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Investigating the relationship between clock gene stability and the pace of the vertebrate segmentation clock
… another Wnt inhibitor XAV939 and a number of cdk inhibitors can phenocopy this effect in the PSM. This effect appears independent of the cell cycle and these inhibitors appear to have a general effect on transcription in the chicken PSM. In contrast to a previous report, we find that direct …
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TRIB3 as an integrator of metabolic stresses: Role in lung cancer progression
… cycle related genes showed an upregulation of CDK inhibitors in (NCI-H358) TRIB3 overexpression cells, while depletion of TRIB3 led to the down-regulation of CDK inhibitors. The upregulation of the CKI p27 was consistent in all cell lines used in this study with overexpressed TRIB3 level. This …
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Characterization of the molecular mechanisms underlying retinoic acid induced growth inhibition in MCF-7 human breast cancer cells.
… a down regulation of cyclin dependent kinase 2 (cdk2) and cyclin D1 gene expression and a profound down regulation of cdk2 activity. In contrast, no changes were seen in cdk4 expression or activity. We have further demonstrated that RA did not cause a change in the overall levels of expression of …
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The nature of cachexia in patients with heart failure and stable coronary artery disease
… activation of tissue cytokines and cell cycle inhibitors. We studied five subject groups. Three were groups of patients with stable coronary artery disease: 1) HF-cachexia - patients with HF, reduced left ventricular systolic function and cachexia, n=10; 2) HF-no cachexia - those with HF, …
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Strukturbiologische Untersuchungen und Faltungsstudien von Modellproteinen mittels NMR-Spektroskopie
… ORF56 aus S. islandicus sowie des humanen CDK-Inhibitors p19INK4d mit einer Reihe biophysikalischer Methoden ausführlich charakterisiert. Die schnelle interne Dynamik von CspB wurde bei verschiedenen Lösungsmittelviskositäten untersucht, wobei durch eine erweiterte Lipari-Szabo-Analyse der …
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A CELL CYCLE CLOCK REGULATES THE EPIGENETIC LANDSCAPE OF AML CELLS AND DETERMINES SENSITIVITY TO LSD1 INHIBITION
… the G1 phase, can sensitize AML cells to LSD1 inhibitors. This is achieved through a novel combinatorial approach involving clinically approved CDK inhibitors, such as Palbociclib, with LSD1 inhibitors. Moreover, the study investigates mechanistically the implications of cell cycle …
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Part I: Design, synthesis, and studies of novel age-inhibitors and age-breakers; Part II: Novel synthetic methods for organofluorine compound
<p>"Novel small molecule inhibitors and breakers of advanced glycation end-products (AGEs) have been synthesized and their <em>in vitro</em> inhibitory activities have been studied by <sup>13</sup>C NMR, fluorescence, and UV-visible spectroscopy. We have demonstrated that these AGE-inhibitors and …
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Posttranscriptional gene silencing of p27 in primary prostate epithelial cells by small inhibitory RNA (siRNA)
… by the intricate interplay of many molecules. Cdks (cyclin dependent kinases), along with cyclins, are major control switches for the cell cycle, causing the cell to move from G1 to S or G2 to M. Their function is tightly regulated by Cdk-inhibitors such as the p21 and p27 Cip/Kip proteins. …
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A SEARCH FOR EPIGENETIC VULNERABILITIES OF AML CELLS PERFORMED BY A CDK INHIBITOR¿BASED CRISPR SCREENING
… of the cell cycle through sub-optimal doses of CDK4/6 inhibitors reprograms the chromatin landscape of fast-cycling AML cells resistant to LSD1 inhibition, rendering them more similar to slow-cycling counterparts that are intrinsically sensitive to LSD1 inhibition. This finding suggested that …
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Peak Mitotic Cyclin Permits Mitotic Exit
… are all regulated by Cyclin-dependent kinase (Cdk). Cyclin/Cdk complexes promote replication origin firing and mitotic entry, and conversely, inhibit pre-replication origin loading and exit from mitosis. Cyclin synthesis and degradation, Cdk phosphorylation and Cdk inhibitors are controlled …
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Controls Over S-Phase And Over Nuclear Synchrony
… We conclude that cyclin dependent kinase (CDK) inhibits re-initiation of a mostly normal S-phase program during G2. To identify features of replication origins important for amplification, we investigated origin firing and local genome amplification in the presence of excess helicase …
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Modulation von Zellzyklus- und Apoptoseregulation in humanen kolorektalen Karzinomzellen durch Butyrat und Acetylsalicylsäure
… Butyrat auf die Expression von p21Waf1/Cip1 und cdk2: Acetylsalicylsäure und Butyrat in höheren Konzentrationen reduzierten die Expression von cdk2 in HT-29 Zellen, in niedrigen Konzentrationen führte nur die Acetylsalicylsäure-Butyrat-Kombination zu einem Abfall des cdk2-Proteingehalts. Butyrat …
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Targeting DNA Double-Strand Break Repair to Potentiate Radio- and Chemo Therapy of Glioblastoma
… in these lines. We have recently shown that CDKs 1 and 2 promote HR in S and G2 phases of the cell cycle, in part, by phosphorylating the exonuclease EXO1. We hypothesized, therefore, that blocking CDKs 1 and 2 might be a viable strategy for re-sensitizing recurrent tumors to TMZ. Indeed, we …
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Low Molecular Weight Cyclin E Deregulates Dna Replication and Damage Repair to Promote Genomic Instability In Breast Cancer
… half-life, higher affinity to its kinase partner CDK2, and resistance to endogenous CDK inhibitors such as p21 and p27 all promote the tumorigenic ability of LMW-E. Clinical studies in breast cancer reveal that overexpression of LMW-E predicts recurrence and poor survival in breast cancer patients …
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