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 “"PI3K inhibitors"”.
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Design, Synthesis, and Screening of Novel Phosphatidylinositol 3-Kinase (PI3K) Inhibitors Activated by Prostate Specific Antigen (PSA): Prodrug Treatment for Androgen-Independent Prostate Cancer
The PI3K/Akt pathway is one of the most frequently dysregulated signaling pathways in cancer and remains a crucial target in drug development. Current therapeutic drugs are potent, but often lack the cellular specificity needed to lower toxicity effects. Here we show the design and synthesis of two …
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SYNTHESIS AND SCREENING OF PI3K INHIBITOR PRODRUGS FOR TREATMENT OF PROSTATE CANCER
… prostate cancer. Phosphoinositide 3-kinases (PI3Ks) are involved in several imperative cellular functions such as growth and survival; therefore, inhibition of PI3K induces apoptosis (programmed cell death) and suppresses tumor growth. Several compounds have been identified as PI3K inhibitors, …
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Cll Metabolism Is Regulated By Prognostic Factors, Modulated By Stroma and Abrogated By Pi3K Inhibition
… a survival benefit to CLL cells, in part through PI3K/AKT pathway. Compared with proliferative B-cell lines, metabolic fluxes of oxygen and lactate were low in quiescent malignant B lymphocytes from CLL patients. Glycolysis (extracellular acidification rate, ECAR) was consistently low in CLL …
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Targeting the protein tyrosine phosphatase, SHP2, and PI3K in FLT3-ITD+ leukemia
… (Y) 768, 955, and/or 969 and that Shp2 and PI3K work cooperatively to promote FLT3-ITD-induced leukemogenesis. Consistently, mutation of N51-FLT3 tyrosine 768 to phenylalanine reduced proliferation and levels of phospho-Erk compared to N51-FLT3-expressing cells while having no effect on …
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Targeting PI3K Isoforms to Improve Effectiveness of T Cells Mediated Immunotherapy
The hyperactivation of the PI3K pathway is associated with immune checkpoint blockade (ICB) resistance in cancer patients, highlighting the potential of combining PI3K inhibitor with ICB. Different PI3K isoforms are suggested to play a role in tumors and T cells, offering an opportunity to …
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Pi3K- and Mtor-Dependent Mechanisms of Lapatinib Resistance and Resulting Therapeutic Opportunities
… resistance. We found that activation of PI3K, specifically the p110α catalytic subunit, was enhanced in two out of three LapR cell lines, through p110α activating mutations and/or upregulation. In a third LapR cell line, mTOR activation was enhanced in a manner independent of its usual …
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Autophagy mechanisms in sputum and peripheral blood cells of patients with severe asthma: a new therapeutic target
… IL-5, IL-1β, and TNF-α. To inhibit autophagy, PI3K inhibitors (LY29400 and 3-methyladenine [3-MA]) and hydroxychloroquine (HCQ) were used. Knockdown of ATG5 and Beclin-1 was performed in A549 cells, and the therapeutic effects of dexamethasone were evaluated. Results: Higher autophagy levels …
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Investigating the isoform-specific role of phosphoinositide 3- kinase p110delta
Phosphoinositide 3-kinases (PI3Ks) are a family of enzymes that regulate a diverse array of biological functions in every cell type by generating lipid second messengers. The PI3K family is comprised of multiple isoforms that are divided into three main classes; class I, II and III. All class I …
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Melatonin-Tamoxifen Drug Conjugates as Breast Cancer Drugs: Pharmacological Evaluation in Phenotypically Diverse Breast Cancer Models and Pharmacokinetic Assessment in Liver Microsome and Female Mouse Models
… of action using selective MEK1/2, MEK5, and PI3K inhibitors. C4 and C5 inhibited TamR MCF-7 cells with equal potency and efficacy and both C4 and C5 inhibited TU-BcX-4IC cell viability. Even though both compounds demonstrated similar inhibitory actions against BC cell viability and migration, …
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Direct Effects of Metformin On Pi3K and Ras Signaling In Endometrial Cancer
… metformin’s effect on cell proliferation, PI3K and Ras-MAPK signaling, and apoptosis. A xenograft mouse model was also used to evaluate the effects of metformin treatment on <em>in vivo</em> tumor growth. These preliminary studies demonstrated that K-Ras mutant cell lines exhibited a …
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A dissection of class I phosphoinositide 3-kinase signalling in mouse embryonic fibroblasts and prostate organoids
Class I PI3Ks are a family (α, β, δ and γ) of ubiquitous lipid kinases that can be activated by cell surface receptors to 3-phosphorylate PI(4,5)P2 (phosphatidylinositol(4,5)-bisphosphate) and generate the signalling lipid PI(3,4,5)P3. The PI(3,4,5)P3 signal then activates a diverse collection of …
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Actions of Pi3K-Delta Inhibitor, Idelalisib, and Its Combination With Bendamustine In Chronic Lymphocytic Leukemia
… a major role in cancer cell growth and survival. PI3K α and β are most studied. PI3K pathway is highly dysregulated in many cancers and aberrant PI3K signaling is associated with oncogene mutations and disease progression in solid tumors and in hematologic malignancies.</p> <p>Chronic lymphocytic …