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 16 of 16 for “"vemurafenib"”.
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Mouse Oocyte Maturation and Embryo Development After Exposure to Vemurafenib (PLX4032), an Anti-Melanoma B-RAF V600E Inhibitor
<p>Vemurafenib is a selective B-Raf<sup>V600E</sup> inhibitor in melanoma targeted therapy which also inhibits the wild type B- and C-Raf. In oocyte maturation, the C-Raf/MAPK pathway acts as an important self-enhancing and promoting system, w hereas in embryo development, the C-Raf/M APK pathway …
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A Phase I Dose-Escalation Study of The Braf Inhibitor Vemurafenib In Combination With The Mtor Inhibitor Everolimus In Subjects With Advanced Cancer
<p>Vemurafenib has been approved in the United States for the treatment of relapsed or refractory BRAF mutation positive malignant melanoma and is being investigated in various other malignancies. The RAS/RAF/MEK/ERK (MAPK) pathway is critical to cell proliferation in many human cancers. The mTOR …
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Overcoming Acquired Resistance to BRAF Inhibitors by Novel Synergistic Drug Combination and Discovery of Novel Smac Mimetics as Selective Survivin Inhibitors
… therapy. Acquired clinical resistance to vemurafenib, a selective BRAFV600E inhibitor, arises frequently after short term chemotherapy. Since the inhibitions of targets in the RAFMEK-ERK pathway result in G0/G1 cell cycle arrest, vemurafenib-resistant cancer cells are expected to escape …
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Procaspase-3 activation as a strategy to overcome resistance to targeted anticancer therapies
… that can be drugged with a BRAFV600E inhibitor vemurafenib. Chapter 3 reports the synergistic activity of PAC-1 + vemurafenib and PAC-1 + vemurafenib + trametinib in enhancing caspase-3 activity and apoptotic cell death in BRAFV600E melanoma cell lines. As a result of increased caspase-3 …
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Investigation of signalling pathways associated with the development of BRAF inhibitor resistance and treatment of melanoma
… α5 and PAI-1 and p21 levels were associated with vemurafenib resistant BRAFV600E melanoma cells and the TGF-β pathway is the major regulator. Combination of cilengitide with vemurafenib, showed a highly synergistic effect and significantly blocked the in-vasive and colony initiating features and …
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Epigenetic Modulation In Braf Mutated Metastatic Colorectal Cancer
… models of BRAFV600E mCRC were treated with vemurafenib or azacitidine, alone or in combination, to assess for changes in tumor size. Tumors and cell lines exposed to azacitidine were analyzed for methylation status and for gene expression differences, with particular emphasis on genes …
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Transient Metabolic Alterations Induced by Chemotherapeutics in Cancer Persisters
… alterations in melanoma cells mediated by Vemurafenib (VEM), a BRAF inhibitor. Co-treatment with BRAF inhibitors is a common treatment strategy for melanoma cancer. However, how a BRAF inhibitor itself alters melanoma cell metabolism and mediates persister survival is not well understood. …
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Roles For Braf Kinase Activating Mutations In Melanoma: Microenvironmental Immunosuppression
… treated with the BRAF(V600E)-specific inhibitor, Vemurafenib, have shown dramatic clinical responses. Here, I show that BRAF(V600E) induces transcription of the IL-1α and IL-1β genes in both melanocytes and melanoma cell lines and that this upregulation is specifically abrogated by targeted …
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Diverse roles for the mitogen-activated protein kinase ERK2 revealed by high-throughput target identification
… of ERK signaling is especially important since vemurafenib, the first pharmaceutical directly targeting the MAPK pathway, has recently been approved to treat advanced melanoma. ERK controls cellular phenotypes by phosphorylating over two hundred known substrate proteins, however new ERK targets …
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Clinical and Therapeutic Significance of Obesity In Melanoma
… therapy [dabrafenib and trametinib (D+T) and vemurafenib and cobimetinib], immunotherapy [ipilimumab and anti-PD-1/PDL-1], and chemotherapy. The functional significance of obesity was tested using a mouse model of diet-induced obesity (DIO) injected subcutaneously with murine melanoma cells. …
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The Oncogenic Map Kinase Signaling Pathway Modulates Mhc-I Surface Expression In Melanoma
… patient survival. Two MAPK targeted inhibitors, vemurafenib and dabrafenib, have produced positive results in clinical trials thus far, but they are not without limitations. Recent studies have shown that oncogene activation in tumor cells can affect the level of expression of major …
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Opportunities and challenges in oncology targeted drug development : an assessment of the use of prevalence and companion diagnostic performance thresholds to guide clinical trial strategies
… to demonstrate benefit. Several drugs, including vemurafenib and crizotinib have demonstrated these benefits along with commercial success. However, significant risk exists for the drug developer since approval may be threatened if they fail to meet unclear and differing yet parallel requirements …
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CHARACTERIZATION OF EPCAM IN THYROID CANCER BIOLOGY BY THREE-DIMENSIONAL SPHEROIDS IN VITRO MODEL.
… drug commonly used in clinical practice, Vemurafenib (PLX-4032), both in FRO and HTCC3 adherent cells, and EpCAM+ cells appeared to be more resistant. Finally, the 3D sphere model is also a valid in vitro approach to assess cell response to PLX-4032 and we observed that FRO-derived 3D …
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An investigation on role of the ATP-binding cassette B5 (ABCB5) transporter as potential mediator of melanoma resistance to BRAF inhibition
… accumulation analyses revealed no reduction in vemurafenib or dabrafenib concentrations, indicating that BRAFis do not act as substrates for ABCB5. Altogether, our studies suggest that ABCB5 expression is linked to the melanocytic program. However, despite the molecular docking evidence that …
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Epigenetic dysregulation of novel candidate genes in melanoma
… Although new melanoma therapies including vemurafenib and ipilimumab confer significant clinical benefit, accumulating evidence suggests that they are less effective when tumour load is high and patient performance status poor, as is often the case in advanced disease. New strategies for …