Global ETD Search
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Showing 1 to 6 of 6 for “"MLN8237"”.
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Identifying and Targeting Molecular Deregulations In Uterine Leiomyosarcoma: A Role For Mtor Inhibition-Based Combination Therapies
… therapy with rapamycin (an mTORC1 inhibitor) and MLN8237 (an investigational Aurk A inhibitor) profoundly and synergistically abrogated ULMS growth <em>in vitro</em>. Interestingly, the superior effects were noted only when MLN8237 was pre-administered. This novel therapeutic combination and …
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Novel combination strategies with Aurora Kinase Inhibitors: using pre-clinical data to guide clinical trial design
… to the drug combination. Combinations of MLN8237 (an AK-A inhibitor) with paclitaxel and docetaxel were studied in a T24 bladder cancer xenograft model, and these confirmed tolerability with evidence of efficacy in tumour growth inhibition. Published clinical trials have now demonstrated …
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Cellular Determinants Of AURKA Degradation By Small Molecule Proteolysis-Targeting Chimeras
… and the emergence of resistance mechanisms. MLN8237 (alisertib) is an example of a high-affinity, selective kinase inhibitor of AURKA which has mostly failed in clinical trials. More recently, kinase-independent functions of AURKA (e.g., oncogenic signalling, transcriptional activation) have …
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The Role of Stromal-Derived Factors in Neuroblastoma Differentiation
… inhibitor decitabine with the AurkA inhibitor MLN8237 enhances differentiation and reduces proliferation compared to either agent alone. Importantly, the combination of clinically achievable doses of these targeted agents dramatically reduces tumor growth in orthotopic xenograft models of …
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A study of novel tools to measure and perturb Aurora Kinase A protein stability
… targeting chimeras (PROTACs) and consisted of MLN8237, a small molecule inhibitor of AurKA, linked to pomalidomide, a chemical ligand for the Cereblon (CRB) E3 ligase. The PROTAC works by ectopically recruiting AurKA to CRB, resulting in its ubiquitination and subsequent degradation by the UPS. …
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Identifying Mechanisms Of Resistance And Potential Therapeutic Targets For Pediatric Acute Myeloid Leukemia
… and one of either the aurora A kinase inhibitor MLN8237, the aurora B kinase inhibitor AZD1152-HQPA, the Plk1 inhibitor BI6237, or the wee1 inhibitor MK-1775. It was found that MK-1775, in contrast to the other three agents, synergized with araC in antiproliferative MTT assays in both cell lines …