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Phase II study of BKM120 in patients with advanced esophageal squamous cell carcinoma (EPOC1303)
BackgroundPI3K/AKT/mTOR pathway is frequently overactive in esophageal squamous cell carcinoma (ESCC), making it an attractive treatment target....
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PI3K inhibition by BKM120 results in anti-proliferative effects on corticotroph tumor cells
PurposeCushing's disease is associated with significant morbidity; thus, additional tumor-directed drugs with the potential to exert antineoplastic...
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A phase Ib study of a PI3Kinase inhibitor BKM120 in combination with panitumumab in patients with KRAS wild-type advanced colorectal cancer
Background Resistance to Epidermal Growth Factor inhibition (EGFRi) in patients with KRAS wild-type (wt) Colorectal Cancer (CRC) may occur as a...
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Dual targeting of MEK and PI3K effectively controls the proliferation of human EGFR-TKI resistant non-small cell lung carcinoma cell lines with different genetic backgrounds
BackgroundMolecular targeted therapy for non-small cell lung carcinoma (NSCLC) is restricted due to resistance to epidermal growth factor receptor...
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Phase I/II study of bevacizumab with BKM120, an oral PI3K inhibitor, in patients with refractory solid tumors (phase I) and relapsed/refractory glioblastoma (phase II)
BackgroundCurrent bevacizumab-based regimens have failed to improve survival in patients with recurrent glioblastoma. To improve treatment efficacy,...
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Linear ubiquitination of PTEN impairs its function to promote prostate cancer progression
PTEN is frequently mutated in human cancers, which leads to the excessive activation of PI3K/AKT signaling and thus promotes tumorigenesis and drug...
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The Superior Cytotoxicity of Dual Targeting of BCR/ABL and PI3K in K562 Cells: Proposing a Novel Therapeutic Potential for the Treatment of CML
Apart from BCR/ABL which is the main player in the pathogenesis of chronic myeloid leukemia (CML), the role of other signaling cascades should not be...
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CUDC-907 exhibits potent antitumor effects against ovarian cancer through multiple in vivo and in vitro mechanisms
PurposeCUDC-907 is a promising dual-target inhibitor of the HDAC and PI3K signaling pathways, with demonstrated therapeutic effects in a range of...
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A Phase Ib/II, open-label, multicenter study of INC280 (capmatinib) alone and in combination with buparlisib (BKM120) in adult patients with recurrent glioblastoma
PurposeTo estimate the maximum tolerated dose (MTD) and/or identify the recommended Phase II dose (RP2D) for combined INC280 and buparlisib in...
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Rationale for the advancement of PI3K pathway inhibitors for personalized chordoma therapy
PurposeChordomas are rare and serious tumors with few effective treatments outside of aggressive surgery and radiation. Targeted therapies may...
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Dual roles of HK3 in regulating the network between tumor cells and tumor-associated macrophages in neuroblastoma
Neuroblastoma (NB) is the most common and deadliest extracranial solid tumor in children. Targeting tumor-associated macrophages (TAMs) is a strategy...
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Recent advances in targeted strategies for triple-negative breast cancer
Triple-negative breast cancer (TNBC), a highly aggressive subtype of breast cancer, negatively expresses estrogen receptor, progesterone receptor,...
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The multifaced role and therapeutic regulation of autophagy in ovarian cancer
Ovarian cancer (OC) is one of the tumors that occurs most frequently in women. Autophagy is involved in cell homeostasis, biomolecule recycling, and...
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PI3K/AKT/mTOR signaling pathway: an important driver and therapeutic target in triple-negative breast cancer
Triple-negative breast cancer (TNBC) is a highly heterogeneous tumor lacking estrogen receptor (ER), progesterone receptor (PR), and human epidermal...
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PI3K-regulated Glycine N-methyltransferase is required for the development of prostate cancer
Glycine N-Methyltransferase (GNMT) is a metabolic enzyme that integrates metabolism and epigenetic regulation. The product of GNMT, sarcosine, has...
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Targeted inhibition of cooperative mutation- and therapy-induced AKT activation in AML effectively enhances response to chemotherapy
Most AML patients exhibit mutational activation of the PI3K/AKT signaling pathway, which promotes downstream effects including growth, survival, DNA...
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Biology of breast cancer brain metastases and novel therapies targeting the blood brain barrier: an updated review
Brain metastasis (BM) is a critical cause of morbidity and mortality in patients with breast cancer (BC). Compared with other cancer cells, BC cells...
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Targeting PI3K/Akt signal transduction for cancer therapy
The phosphatidylinositol 3-kinase (PI3K)/Akt pathway plays a crucial role in various cellular processes and is aberrantly activated in cancers,...
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Resistance to Poly (ADP-Ribose) Polymerase Inhibitors (PARPi): Mechanisms and Potential to Reverse
Purpose of ReviewThis review will focus on the most common mechanisms for poly (ADP-ribose) polymerase inhibitors’ (PARPi) resistance and the main...
