AKT inhibitor
Additive effect by combination of Akt inhibitor, MK-2206, and PDGFR inhibitor, tyrphostin AG 1296, in suppressing anaplastic thyroid carcinoma cell viability and motility
... an Akt inhibitor and a novel PDGFR inhibitor in cell survival, apoptosis, cell signaling pathways, cell migration, and invasion in vitro, as well as tumor growth in vivo in ...of Akt signaling ...
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The AKT Inhibitor MK-2206 is Cytotoxic in Hepatocarcinoma Cells Displaying Hyperphosphorylated AKT-1 and Synergizes with Conventional Chemotherapy
... allosteric Akt inhibitor, ...multikinase inhibitor Sorafenib and MK-2206 overcame the resistance of HCC cells to Sorafenib at clinically achievable concentrations, suggesting the potential use of ...
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Akt Inhibitor Akt-IV Blocks Virus Replication through an Akt-Independent Mechanism
... the inhibitor Akt-IV displays a mechanism of action that is different from what has been described previously and suggest that this compound deserves further study as a broad-spectrum antiviral ...the ...
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Novel B55α-PP2A mutations in AML promote AKT T308 phosphorylation and sensitivity to AKT inhibitor-induced growth arrest
... or AKT pathway has been shown to correlate with acute myeloid leukemia (AML) ...dephosphorylate AKT at Thr-308 rendering it ...the AKT inhibitor MK2206, but less responsive to the PP2A ...
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Phase II trial of AKT inhibitor MK 2206 in patients with advanced breast cancer who have tumors with PIK3CA or AKT mutations, and/or PTEN loss/PTEN mutation
... novel AKT inhibitors including allosteric inhibitors ARQ092, BAY1125976, TAS-117, catalytic inhibitors AZD5363, ipatasertib, GSK2141795, and the dual AKT/ S6K inhibitor ...with AKT alterations ...
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A Phase I Open-Label Study to Identify a Dosing Regimen of the Pan-AKT Inhibitor AZD5363 for Evaluation in Solid Tumors and in PIK3CA-Mutated Breast and Gynecologic Cancers.
... other AKT inhibitors, such as the allosteric inhibitor MK2206 or kinase inhibitors such as GSK2141795 and ipatasertib (GDC-0068) (1, ...on AKT, a key regulator of glucose transport and metabolism in ...
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A putative biomarker signature for clinically effective AKT inhibition: correlation of in vitro in vivo and clinical data identifies the importance of modulation of the mTORC1 pathway
... of AKT in platinum- resistant cells occurs by phosphorylation of AKT at serine 473 by DNA-dependent protein kinase (DNA- PK) [5] following DNA damage, directly linking the established role of AKT in ...
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<p>ARHGAP10 Inhibits the Proliferation and Metastasis of CRC Cells via Blocking the Activity of RhoA/AKT Signaling Pathway</p>
... Previous report has demonstrated that the activation of PI3K/AKT acts as an upstream signal in SOX2-induced MMP-2 expression in Hep-2 cells. 27 Moreover, inhibiting the activity of PI3K/AKT signaling ...
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Targeting Akt by SC66 triggers GSK-3β mediated apoptosis in colon cancer therapy
... enhances Akt ubiquitination and its deactivation in both HeLa and HEK293T cells ...the AKT signaling pathway [8]. And the novel Akt inhibitor SC66 directly deactivated Akt and ...
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CHARACTERIZING QUIESCENCE AND AUTOPHAGY AS FEATURES OF DORMANCY IN METASTATIC OVARIAN CANCER CELLS
... allosteric AKT inhibitor) with autophagy blockade synergistically compromises cell ...the AKT inhibitor MK-2206 (an analog of Akti-1/2), is currently undergoing clinical trials in patients ...
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Cellular stress-induced up-regulation of FMRP promotes cell survival by modulating PI3K-Akt phosphorylation cascades
... vate Akt by phosphorylation at Ser473 and Thr308, which leads to the modulation of Bad, caspase 9, and transcription factors including forkhead family and NF- kB ...functional Akt activity was necessary for ...
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Integrating a Next Generation Sequencing Panel into Clinical Practice in Ovarian Cancer
... Results: Of the 84 patients, 55 (65.1%) had high-grade serous carcinomas. Seventy-three (86.7%) patients underwent NGS at the time of diagnosis, and 11 (13.3%) underwent NGS upon relapse. The most common genetic ...
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Modulating effect of the PI3-kinase inhibitor LY294002 on cisplatin in human pancreatic cancer cells
... signaling inhibitor of the PI3K/Akt path- way, can modulate sensitivity to cancer chemotherapy in ...that Akt activity might promote therapeutic resistance in human non- small cell lung cancer cells ...
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Mitomycin C treatment induces resistance and enhanced migration via phosphorylated Akt in aggressive lung cancer cells
... phosphorylated Akt (p-Akt) were higher in CL1-5 cells. Administering a p-Akt inhibitor reduced the MMC resistance, demonstrating that p-Akt is important in the MMC resistance of CL1-5 ...
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Ibrutinib suppresses LPS-induced neuroinflammatory responses in BV2 microglial cells and wild-type mice
... Microglial cell migration is associated with stimulation of microglial cells, which causes chronic inflammation and neuronal damage [48]. For example, chemokines released from microglial cells are key components required ...
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The transcription factor MITF is a critical regulator of GPNMB expression in dendritic cells
... of Akt inhibition, we per- formed T cell proliferation (MLR) ...with Akt inhibitor or ima- tinib resulted in significantly reduced capacity to stimulate proliferation of allogeneic T cells to an ...
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Functional significance of the signal transduction pathways Akt and Erk in ovarian follicles: in vitro and in vivo studies in cattle and sheep
... the Akt and Erk pathways would decrease fol- licle growth and oestradiol production by ovine ovarian follicles in ...DMSO), Akt inhibitor (n = 5; follicle injected with LY294002 in control medium), ...
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Hepatocellular carcinoma-derived exosomal miRNA-21 contributes to tumor progression by converting hepatocyte stellate cells to cancer-associated fibroblasts
... Our results indicated that tumor-derived exosomal miRNA-21 could convert HSCs to CAFs by decreasing PTEN, leading to activated PDK1/AKT signaling path- way in HCC. In addition, CAFs exhibited increased se- cretion ...
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EGFR blockade prevents glioma escape from BRAF V600E targeted therapy
... Proteins were extracted from cells and tissues using cell lysis buffer (Cell Signaling) supplemented with proteinase (Roche) and phosSTOP phosphatase inhibitor cocktail (Roche). Proteins were separated by SDS-PAGE ...
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Opposite regulation by PI3K/Akt and MAPK/ERK pathways of tissue factor expression, cell-associated procoagulant activity and invasiveness in MDA-MB-231 cells
... In agreement with other reports [7,8], an essential role of PI3K/Akt in TF expression in MDA-MB-231 cells was found because treatment by either LY294002 or wort- mannin decreased TF expression in a dose-dependent ...
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