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 12 of 12 for “"roscovitine"”.
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Somatic cell interspecies nuclear transfer
… diameter) follicles were either pretreated with roscovitine or placed in maturation (IVM only) prior to NT. Roscovitine pretreatment did not improve nuclear maturation rates (roscovitine pretreatment 57% vs. IVM only 66%) and no fusion was obtained from roscovitine-pretreated oocytes after NT. …
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Design and Synthesis of Benzimidazoles as CDK5 Inhibitors and Progress toward the Total Synthesis of Tubulysin D
… of the known non-selective CDK5 inhibitor (R)-Roscovitine were designed. Synthesis of 6-benzyl substituted benzimidazole analogs was developed and two compounds were synthesized in this series. Two methods of the synthesis of 6-(2-hydroxy-1-alkyl)amino substituted benzimidazole analogs were …
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Design and Synthesis of CDK-5 and MEK-5 Inhibitors and Synthesis towards Tubulysin Analogs
… and phenylacetamide benzimidazoles based on (R)-Roscovitine, a non-selective inhibitor of CDK-5 were designed and synthesized. </p><p>MEK-5, a member of the MAPK family, phosphorylates ERK-5 permitting cells to survive oxidative stress. MEK-5 is upregulated in tumor cells and activated by …
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Design and Synthesis of Novel Benzimidazoles and Aminothiazoles as Small Molecule Inhibitors of CDK5/p25
… of CDK5/p25 with a non-selective CDK inhibitor R-Roscovitine (PDB ID: 1UNL), eight series of novel compounds with a benzimidazole core were designed, synthesized and tested as inhibitors of CDK5/p25. An efficient synthesis of trisubtituted benzimidazoles was developed to explore the SAR at the 1-, …
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Synthetic Lethality of Cdk Inhibition and Doxorubicin In Triple-Negative Breast Cancer Requires P53 Inactivation
… administration of the pan-CDK inhibitor roscovitine prior to doxorubicin treatment is synthetic lethal explicitly in TNBC cells. Furthermore, this novel combination therapy is well tolerated and efficacious, significantly reducing tumor volume and increasing overall survival compared to …
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A functional and therapeutic investigation of ciliopathy proteins and ciliopathies
… Administration of two drugs, Rapamycin and Roscovitine, were sufficient to rescue formation of kidney cysts and restore the filterative capacity of the kidney. This paves the way for studies in mouse models and, ultimately, in humans, where no treatment for ciliopathic renal disease exists. …
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Engineering of polyphenol metabolism in tomatoes to enhance anti-cancer activities
… with the chemotherapeutic agents, doxorubicin or roscovitine, and high-anthocyanin or -resveratrol tomato extracts showed that dietary polyphenols might potentiate the effects of pharmacological agents in vitro. This work demonstrated that the health benefits of dietary plants can be significantly …
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Quantitative analysis of signaling networks in proneural glioblastoma
… response was abrogated by inhibiting CDK₁ with roscovitine, a CDK inhibitor, demonstrating the necessity of active CDK₁ for MK-₁₇₇₅ induced mitotic catastrophe. To assess the extensibility of targeting Wee₁ and the G₂/M checkpoint in GBM, we treated patientderived xenograft (PDX) cell lines with …
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Protein Phosphatase Inhibitor-1 and Cdk5: Of Molecules and Memory
… by pharmacological inhibition of Cdk5 with roscovitine. Finally, in a related study, we helped firmly establish a role for Cdk5 in hippocampal synaptic plasticity by demonstrating that conditional loss of Cdk5 enhances NMDA receptor-mediated currents, particularly of the NR2B type.
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Lmw-E Mediates Mammary Tumorigenesis By Deregulating Acinar Morphogenesis & Generating Cancer Stem Cells
… patient survival. Combination treatment using roscovitine</p> <p>(CDK inhibitor) plus either rapamycin (mTOR inhibitor) or sorafenib (b-raf inhibitor)</p> <p>effectively prevented aberrant acinar formation in LMW-E-expressing cells by</p> <p>inducing the G1/S cell cycle arrest. In addition, the …
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Targeting DNA Double-Strand Break Repair to Potentiate Radio- and Chemo Therapy of Glioblastoma
… we found that CDK inhibitors, AZD5438 and Roscovitine, could attenuate HR in the recurrent TMZ-resistant cell lines resulting in significant chemo-sensitization to TMZ. While HR is primarily involved in the repair of TMZ-induced DSBs, ionizing radiation induced DSBs would be mainly repaired …
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Investigating Checkpoint Kinases 1/2 As Novel Therapeutic Targets In Head and Neck Squamous Cell Carcinoma
… cells and that loss of cdk2 or treatment with Roscovitine rescues the lethal phenotype seen in the sensitive cells upon Chk1 inhibition. These results suggest that exquisite sensitivity to Chk1 inhibition in a subset of HNSCC cells could be due to these cells being in a pre-existing state of …