DESIGN AND SYNTHESIS OF NEW EGFR- TYROSINE KINASE INHIBITORS CONTAINING PYRAZOLO[3,4-d]PYRIMIDINE CORES AS ANTICANCER AGENTS

2012 ◽  
Vol 35 (1) ◽  
pp. 27-42 ◽  
Author(s):  
Rania Bakr ◽  
Eman Abdelall ◽  
Mohamed Abdel-Hamid ◽  
Manal Kandeel
Keyword(s):  
Tyrosine Kinase ◽  
Tyrosine Kinase Inhibitors ◽  
Anticancer Agents ◽  
Kinase Inhibitors ◽  
Design And Synthesis ◽  
Egfr Tyrosine Kinase ◽  
Egfr Tyrosine Kinase Inhibitors

scholarly journals Drug Tolerance to EGFR Tyrosine Kinase Inhibitors in Lung Cancers with EGFR Mutations

Cells ◽  
2021 ◽  
Vol 10 (7) ◽  
pp. 1590
Author(s):  
Kenichi Suda ◽  
Tetsuya Mitsudomi
Keyword(s):  
Lung Cancer ◽  
Tyrosine Kinase ◽  
Tyrosine Kinase Inhibitors ◽  
Molecular Mechanisms ◽  
Kinase Inhibitors ◽  
Drug Tolerance ◽  
Lung Cancers ◽  
Egfr Tyrosine Kinase ◽  
Egfr Tyrosine Kinase Inhibitors ◽  
Egfr Mutated

Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs) serve as the standard of care for the first-line treatment of patients with lung cancers with EGFR-activating mutations. However, the acquisition of resistance to EGFR TKIs is almost inevitable, with extremely rare exceptions, and drug-tolerant cells (DTCs) that demonstrate reversible drug insensitivity and that survive the early phase of TKI exposure are hypothesized to be an important source of cancer cells that eventually acquire irreversible resistance. Numerous studies on the molecular mechanisms of drug tolerance of EGFR-mutated lung cancers employ lung cancer cell lines as models. Here, we reviewed these studies to generally describe the features, potential origins, and candidate molecular mechanisms of DTCs. The rapid development of an optimal treatment for EGFR-mutated lung cancer will require a better understanding of the underlying molecular mechanisms of the drug insensitivity of DTCs.

scholarly journals V843I, a Lung Cancer Predisposing EGFR Mutation, Is Responsible for Resistance to EGFR Tyrosine Kinase Inhibitors

2014 ◽  
Vol 9 (9) ◽  
pp. 1377-1384 ◽  
Author(s):  
Satsuki Matsushima ◽  
Kouki Ohtsuka ◽  
Hiroaki Ohnishi ◽  
Masachika Fujiwara ◽  
Hiroyuki Nakamura ◽  
...  
Keyword(s):  
Lung Cancer ◽  
Tyrosine Kinase ◽  
Tyrosine Kinase Inhibitors ◽  
Kinase Inhibitors ◽  
Egfr Mutation ◽  
Egfr Tyrosine Kinase ◽  
Egfr Tyrosine Kinase Inhibitors
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