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Plantamajoside alleviates hypoxia-reoxygenation injury through integrin-linked kinase/c-Src/Akt and the mitochondrial apoptosis signaling pathways in H9c2 myocardial cells
Myocardial ischemia–reperfusion injury(MIRI) is one of the common complications after myocardial infarction surgery, Oxidative stress is among the...
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c-Src facilitates tumorigenesis by phosphorylating and activating G6PD
Glucose-6-phosphate dehydrogenase (G6PD) is the first and rate-limiting enzyme in pentose phosphate pathway (PPP), excessive activation of which has...
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Inhibitor of protein kinase N3 suppresses excessive bone resorption in ovariectomized mice
IntroductionThe long-term inhibition of bone resorption suppresses new bone formation because these processes are coupled during physiological bone...
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p53 modulates kinase inhibitor resistance and lineage plasticity in NF1-related MPNSTs
Malignant peripheral nerve sheath tumors (MPNSTs) are chemotherapy resistant sarcomas that are a leading cause of death in neurofibromatosis type 1...
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Dasatinib: a potential tyrosine kinase inhibitor to fight against multiple cancer malignancies
Dasatinib is the 2nd generation TKI (Tyrosine Kinase Inhibitor) having the potential to treat numerous forms of leukemic and cancer patients and it...
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Which Second-Line Tyrosine Kinase Inhibitor(s) for Chronic Myeloid Leukemia?
In patients with chronic myeloid leukemia who require second-line tyrosine kinase inhibitor therapy, many options exist. These treatments include...
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First-in-class inhibitor of HSP110 blocks BCR activation through SYK phosphorylation in diffuse large B-cell lymphoma
Activated B-cell-like diffuse large B-cell lymphoma (ABC-DLBCL) is driven by aberrant activation of the B-cell receptor (BCR) and the TLR/MyD88...
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Aromatase inhibition plus/minus Src inhibitor saracatinib (AZD0530) in advanced breast cancer therapy (ARISTACAT): a randomised phase II study
PurposeThe development of oestrogen resistance is a major challenge in managing hormone-sensitive metastatic breast cancer. Saracatinib (AZD0530), an...
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Sitravatinib is a potential EGFR inhibitor and induce a new death phenotype in Glioblastoma
Glioblastoma (GBM) is a highly lethal neurological tumor that presents significant challenge for clinicians due to its heterogeneity and high...
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Antitumor effect of a small-molecule inhibitor of KRASG12D in xenograft models of mucinous appendicular neoplasms
Pseudomyxoma peritonei (PMP) is a rare disease characterized by a massive accumulation of mucus in the peritoneal cavity. The only effective...
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A first-in-human phase I trial of daily oral zelenirstat, a N-myristoyltransferase inhibitor, in patients with advanced solid tumors and relapsed/refractory B-cell lymphomas
Myristoylation, the N-terminal addition of the fatty acid myristate to proteins, regulates membrane-bound signal transduction pathways important in...
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Functional roles of SRC signaling in pancreatic cancer: Recent insights provide novel therapeutic opportunities
Pancreatic ductal adenocarcinoma (PDAC) is an aggressive malignant disease with a 5-year survival rate of <10%. Aberrant activation or elevated...
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Cytotoxicity of combinations of the pan-KRAS SOS1 inhibitor BAY-293 against pancreatic cancer cell lines
KRAS is mutated in approximately 25% of cancer patients and first KRAS G12C-specific inhibitors showed promising responses. Pancreatic cancer has the...
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Targeting PELP1 oncogenic signaling in TNBC with the small molecule inhibitor SMIP34
PurposeTriple-negative breast cancer (TNBC) is the most aggressive subtype of breast cancer. Oncogenic PELP1 is frequently overexpressed in TNBC, and...
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Epigenetic reprogramming of cell cycle genes by ACK1 promotes breast cancer resistance to CDK4/6 inhibitor
Hormone receptor-positive, HER2-negative advanced breast cancers exhibit high sensitivity to CDK4/6 inhibitors such as palbociclib. However, most...
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Comparative biochemical kinase activity analysis identifies rivoceranib as a highly selective VEGFR2 inhibitor
Vascular endothelial growth factor receptor 2 (VEGFR2), a key regulator of tumor angiogenesis, is highly expressed across numerous tumor types and...
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Synergistic cytotoxicity of the CDK4 inhibitor Fascaplysin in combination with EGFR inhibitor Afatinib against Non-small Cell Lung Cancer
In the absence of suitable molecular markers, non-small cell lung cancer (NSCLC) patients have to be treated with chemotherapy with poor results at...
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Src inhibitor dasatinib sensitized gastric cancer cells to cisplatin
Gastric cancer (GC) is characterized by high incidence and mortality, and lacks effective treatment. Surgery, combined with chemo- and radiation...
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The dual HCK/BTK inhibitor KIN-8194 impairs growth and integrin-mediated adhesion of BTKi-resistant mantle cell lymphoma
Although Bruton’s tyrosine kinase (BTK) inhibitors (BTKi) have significantly improved patient prognosis, mantle cell lymphoma (MCL) is still...
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A small-molecule pan-HER inhibitor alone or in combination with cisplatin exerts efficacy against nasopharyngeal carcinoma
The abnormal activation of HER family kinase activity is closely related to the development of human malignancies. In this study, we used HER kinases...