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The ribosomal protein S6 kinase alpha-1 (RPS6KA1) induces resistance to venetoclax/azacitidine in acute myeloid leukemia
Venetoclax/azacitidine combination therapy is effective in acute myeloid leukemia (AML) and tolerable for older, multimorbid patients. Despite...
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The Role of p90 Ribosomal S6 Kinase (RSK) in Tyrosine Kinase Inhibitor (TKI)-Induced Cardiotoxicity
Targeted therapy, such as tyrosine kinase inhibitors (TKIs), has been approved to manage various cancer types. However, TKI-induced cardiotoxicity is...
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Alteration of Trop-2 expression in breast cancer cells by clinically used therapeutic agents and acquired tamoxifen resistance
BackgroundSacituzumab govitecan is an antibody–drug conjugate that delivers SN-38, an active metabolite of irinotecan, to the target molecule,...
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The role of the p90 ribosomal S6 kinase family in prostate cancer progression and therapy resistance
Prostate cancer (PCa) is the second most commonly occurring cancer in men, with over a million new cases every year worldwide. Tumor growth and...
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Holistic anti-tumor resistance mechanism of YBX1 and its potential as a chemoresistance target in pancreatic ductal adenocarcinoma
The overall survival rate of pancreatic ductal adenocarcinoma (PDAC) is the worst among all cancers, which is mainly due to the fact that most...
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Discovery of a novel dual-target inhibitor against RSK1 and MSK2 to suppress growth of human colon cancer
Colon cancer is the most aggressive tumor in both men and women globally. As many the chemotherapeutic regimens have adverse side effects and...
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YB-1 activating cascades as potential targets in KRAS-mutated tumors
Y‑box binding protein‑1 (YB-1) is a multifunctional protein that is highly expressed in human solid tumors of various entities. Several cellular...
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The mechanisms and reversal strategies of tumor radioresistance in esophageal squamous cell carcinoma
Esophageal squamous cell carcinoma (ESCC) is one of most lethal malignancies with high aggressive potential in the world. Radiotherapy is used as one...
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An overview of kinase downregulators and recent advances in discovery approaches
Since the clinical approval of imatinib, the discovery of protein kinase downregulators entered a prosperous age. However, challenges still exist in...
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Molecular genetics and cellular events of K-Ras-driven tumorigenesis
Cellular transformation and the accumulation of genomic instability are the two key events required for tumorigenesis. K-Ras (Kirsten-rat sarcoma...
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Molecular modeling and structure-based drug discovery approach reveals protein kinases as off-targets for novel anticancer drug RH1
Potential drug target identification and mechanism of action is an important step in drug discovery process, which can be achieved by biochemical...
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Antitumor effects of BI-D1870 on human oral squamous cell carcinoma
PurposeAmong the signaling pathways implicated in the tumorigenesis of oral squamous cell carcinoma (OSCC) is the extracellular signal-regulated...
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mTORC1 upregulation via ERK-dependent gene expression change confers intrinsic resistance to MEK inhibitors in oncogenic KRas-mutant cancer cells
Cancer cells harboring oncogenic BRaf mutants, but not oncogenic KRas mutants, are sensitive to MEK inhibitors (MEKi). The mechanism underlying the...
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RSK2 regulates endocytosis of FGF receptor 1 by phosphorylation on serine 789
FGFR1 (fibroblast growth factor receptor 1) regulates many key cellular responses including proliferation, migration and differentiation through...
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RSK promotes G2/M transition through activating phosphorylation of Cdc25A and Cdc25B
Activation of the mitogen-activated protein kinase (MAPK) cascade in mammalian cell lines positively regulates the G2/M transition. The molecular...
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RSK promotes G2 DNA damage checkpoint silencing and participates in melanoma chemoresistance
The incidence of malignant melanoma is growing rapidly worldwide and there is still no effective therapy for metastatic disease. This type of cancer...
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MKNK1 is a YB-1 target gene responsible for imparting trastuzumab resistance and can be blocked by RSK inhibition
Trastuzumab (Herceptin) resistance is a major obstacle in the treatment of patients with HER2-positive breast cancers. We recently reported that the...
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RSK regulates activated BRAF signalling to mTORC1 and promotes melanoma growth
The Ras/mitogen-activated protein kinase (MAPK) signalling cascade regulates various biological functions, including cell growth, proliferation and...
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YB-1 evokes susceptibility to cancer through cytokinesis failure, mitotic dysfunction and HER2 amplification
Y-box binding protein-1 (YB-1) expression in the mammary gland promotes breast carcinoma that demonstrates a high degree of genomic instability. In...
