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A macrocyclic kinase inhibitor overcomes triple resistant mutations in EGFR-positive lung cancer
Brigatinib-based therapy was effective against osimertinib-resistant EGFR C797S mutants and is undergoing clinical studies. However, tumor relapse...
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SPRY4 inhibits and sensitizes the primary KIT mutants in gastrointestinal stromal tumors (GISTs) to imatinib
BackgroundKIT is frequently mutated in gastrointestinal stromal tumors (GISTs), and the treatment of GISTs largely relies on targeting KIT currently....
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Phospho PTEN mediated dephosphorylation of mitotic kinase PLK1 and Aurora Kinase A prevents aneuploidy and preserves genomic stability
PTEN, dual phosphatase tumor suppressor protein, is found to be frequently mutated in various cancers. Post-translational modification of PTEN is...
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Mouse mutants in schizophrenia risk genes GRIN2A and AKAP11 show EEG abnormalities in common with schizophrenia patients
Schizophrenia is a heterogeneous psychiatric disorder with a strong genetic basis, whose etiology and pathophysiology remain poorly understood. Exome...
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Serine-arginine protein kinase 1 (SRPK1) promotes EGFR-TKI resistance by enhancing GSK3β Ser9 autophosphorylation independent of its kinase activity in non-small-cell lung cancer
Resistance to epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs) is a major challenge for clinicians and patients with...
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Biological and targeting differences between the rare KRAS A146T and canonical KRAS mutants in gastric cancer models
BackgroundGastric cancer (GC) is the third leading cause of cancer-related death worldwide, with a poor prognosis for patients with advanced disease....
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Josephin domain containing 2 (JOSD2) promotes lung cancer by inhibiting LKB1 (Liver kinase B1) activity
Non-small cell lung cancer (NSCLC) ranks as one of the leading causes of cancer-related deaths worldwide. Despite the prominence and effectiveness of...
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Mitochondrial creatine kinase 1 regulates the cell cycle in non-small cell lung cancer via activation of cyclin-dependent kinase 4
BackgroundNon-small cell lung cancer (NSCLC) is the main type of the most common malignant tumor in the world. Previous studies have shown that the...
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Inactivation of kindlin-3 increases human melanoma aggressiveness through the collagen-activated tyrosine kinase receptor DDR1
The role of the focal adhesion protein kindlin-3 as a tumor suppressor and its interaction mechanisms with extracellular matrix constitute a major...
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B-lymphoid tyrosine kinase-mediated FAM83A phosphorylation elevates pancreatic tumorigenesis through interacting with β-catenin
Abnormal activation of Wnt/β-catenin-mediated transcription is closely associated with the malignancy of pancreatic cancer. Family with sequence...
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EBF1–JAK2 inhibits the PAX5 function through physical interaction with PAX5 and kinase activity
Gene aberrations of B-cell regulators and growth signal components such as the JAK–STAT pathway are frequently found in B-cell acute lymphoblastic...
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Prediction of Resistance Mutations Against Upcoming Anaplastic Lymphoma Kinase Inhibitors
BackgroundChromosomal aberrations involving the anaplastic lymphoma kinase (ALK) gene have been observed in approximately 4% of patients with...
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Deoxyguanosine kinase mutation F180S is associated with a lean phenotype in mice
BackgroundDeoxyguanosine kinase (DGUOK) deficiency is one of the genetic causes of mitochondrial DNA depletion syndrome (MDDS) in humans, leading to...
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Tyrosine Kinase Inhibitor Discontinuation in Chronic Myeloid Leukemia: Strategies to Optimize Success and New Directions
Purpose of ReviewThe discovery that patients suffering from chronic myeloid leukemia who obtain deep and long-lasting molecular responses upon...
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SARS-CoV-2 hijacks cellular kinase CDK2 to promote viral RNA synthesis
The coronavirus disease 2019 (COVID-19) pandemic has devastated global health. Identifying key host factors essential for SARS-CoV-2 RNA replication...
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Kinase Fusion–Related Thyroid Carcinomas: Towards Predictive Models for Advanced Actionable Diagnostics
The past decade has brought significant advances in our understanding of the molecular mechanisms of thyroid carcinogenesis. Among thyroid...
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Regulation of proton partitioning in kinase-activating acute myeloid leukemia and its therapeutic implication
Gain-of-function kinase mutations are common in AML and usually portend an inferior prognosis. We reported a novel mechanism whereby kinase mutants...
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The role of liver kinase B1 in tumor progression through regulation of lipid metabolism
The somatic mutation of liver kinase B1 (LKB1) has been implicated in various tumors, which is reflected in the survival, proliferation, and...
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Maximizing the Value of Chronic Myeloid Leukemia Management Using Tyrosine Kinase Inhibitors in the USA: Potential Determinants and Consequences of Healthcare Resource Utilization and Costs, with Proposed Optimization Approaches
Background and ObjectivesThe introduction and widespread use of effective and well-tolerated tyrosine kinase inhibitors for chronic myeloid leukemia...
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Tet methylcytosine dioxygenase 2 (TET2) deficiency elicits EGFR-TKI (tyrosine kinase inhibitors) resistance in non-small cell lung cancer
Despite epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKI) have shown remarkable efficacy in patients with EGFR -mutant...