Tyrosine kinase inhibitors (TKIs) revolutionized the treatment of patients with advanced or metastatic non-small cell lung cancer (NSCLC) harboring most driver gene alterations. Starting from the first generation, research rapidly moved to the development of newer, more selective gener...
MET amplifications, IGF1R activation, etc. The convergent activation of mitogen-activated protein kinase (MAPK) pathway was also proposed to mediate the resistance of TRK inhibition. Second-generation TRK inhibitors are ineffective against off-target resistance, whereas...
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Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs) are current standard of care for patients with EGFR mutation and metastatic non-small-cell lung carcinoma (NSCLC), but most patients using EGFR TKIs acquire resistance later. So, overcoming resistance of EGFR TKIs has become...
We have built up a pharmacophore model of the ATP-binding site of the epidermal growth factor receptor (EGFR) kinase and used it for the rational design of kinase inhibitors. Several examples of the successful use of this model are presented in this review. Amongst these, 4-substituted...
tyrosine kinase inhibitors (TKIs), target-specific inhibitors of PTKs, have been used in treating malignant tumors and play a significant role in targeted therapy of cancer. Currently, drug resistance is the main reason for limiting TKIs efficacy of cancer. The increasing studies indicated that tumo...
Background Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs) represent a highly effective treatment for advanced non-small-cell lung cancer (NSCLC) with active mutations of the EGFR gene. However, most patients develop acquired resistance to EGFR-TKIs. The T790M mutation has...
Tyrosine kinases A tyrosine kinase is an enzyme that can transfer a phosphate group from ATP to a protein in a cell Search Home Air Therapy. Posted onDecember 17, 2024 Reply In summary, this research provides insights and views for future analysis on electrolyte design at large conditions. ...
Lam2, Steve C. F. Au-Yeung1 & Kenneth K. W. To2 Three molecular targeted tyrosine kinase inhibitors (TKI) were conjugated to classical platinum- based drugs with an aim to circumvent TKI resistance, predominately mediated by the emergence of secondary mutations on oncogenic ...
Importantly, tyrosine kinase inhibitors, including SKI606, are currently used for the treatment of some cancers18. However, these drugs have adverse effects on male fertility12. We show here that tyrosine kinase inhibition with SKI606 induced axiopodia retraction in BCs. Our study, thus, provides...