Article
Irreversible inhibitors of the EGF receptor may circumvent acquired resistance to gefitinib.
Proceedings of the National Academy of Sciences of the United States of America - 24 May 2005
Kwak Eunice L, Sordella Raffaella, Bell Daphne W, Godin-Heymann Nadia, Okimoto Ross A, Brannigan Brian W, Harris Patricia L, Driscoll David R, Fidias Panos, Lynch Thomas J, Rabindran Sridhar K, McGinnis John P, Wissner Allan, Sharma Sreenath V, Isselbacher Kurt J, Settleman Jeffrey, Haber Daniel A
Abstract excerpt
Non-small cell lung cancers (NSCLCs) with activating mutations in the kinase domain of the epidermal growth factor receptor (EGFR) demonstrate dramatic, but transient, responses to the reversible tyrosine kinase inhibitors gefitinib (Iressa) and erlotinib (Tarceva). Some recurrent tumors have a common secondary mutation in the EGFR kinase domain, T790M, conferring drug resistance, but in other cases the mechanism...
Topics
- Aminoquinolines
- Aniline Compounds
- Base Sequence
- Carcinoma, Non-Small-Cell Lung
- Cell Proliferation
- Drug Resistance
- ErbB Receptors
- Erlotinib Hydrochloride