Article
The T790M "gatekeeper" mutation in EGFR mediates resistance to low concentrations of an irreversible EGFR inhibitor.
Molecular cancer therapeutics - 1 Apr 2008
Godin-Heymann Nadia, Ulkus Lindsey, Brannigan Brian W, McDermott Ultan, Lamb Jennifer, Maheswaran Shyamala, Settleman Jeffrey, Haber Daniel A
Abstract excerpt
Patients with non-small cell lung cancer (NSCLC) harboring activating mutations in the epidermal growth factor receptor (EGFR) kinase domain tend to respond well to the tyrosine kinase inhibitors, gefitinib and erlotinib. However, following clinical response, these patients typically relapse within a year of treatment. In many cases, resistance is caused by an acquired secondary EGFR kinase domain mutation,...
Topics
- Animals
- Antineoplastic Agents
- Carcinoma, Non-Small-Cell Lung
- Cell Proliferation
- Cells, Cultured
- Drug Resistance, Neoplasm
- ErbB Receptors
- Erlotinib Hydrochloride
- Gefitinib
- Humans
- Immunoblotting
- Lung Neoplasms
- Mice