Activity of the Dual Kinase Inhibitor Lapatinib (GW572016) against HER-2-Overexpressing and Trastuzumab-Treated Breast Cancer Cells
Mayo Clinic · University of California, Los Angeles · +4 more institutions
Abstract
Lapatinib (GW572016) is a selective inhibitor of both epidermal growth factor receptor (EGFR) and HER-2 tyrosine kinases. Here, we explore the therapeutic potential of lapatinib by testing its effect on tumor cell growth in a panel of 31 characterized human breast cancer cell lines, including trastuzumab-conditioned HER-2-positive cell lines. We further characterize its activity in combination with trastuzumab and analyze whether EGFR and HER-2 expression or changes induced in the activation of EGFR, HER-2, Raf, AKT, or extracellular signal-regulated kinase (ERK) are markers of drug activity. We report that concentration-dependent antiproliferative effects of lapatinib were seen in all breast cancer cell lines…
Citation impact
- FWCI
- 33.37
- Percentile
- 100%
- References
- 50
Authors
15- GEGottfried E. KonecnyCorresponding
Mayo Clinic, University of California, Los Angeles, UCLA Jonsson Comprehensive Cancer Center
- MDMark D. Pegram
University of California, Los Angeles, UCLA Jonsson Comprehensive Cancer Center
- NVNatarajan Venkatesan
University of California, Los Angeles, UCLA Jonsson Comprehensive Cancer Center
- RSRichard S. Finn
University of California, Los Angeles, UCLA Jonsson Comprehensive Cancer Center
- GYGuorong Yang
University of California, Los Angeles, UCLA Jonsson Comprehensive Cancer Center
Topics & keywords
- Lapatinib
- Trastuzumab
- Protein kinase B
- Medicine
- Tyrosine-kinase inhibitor
- Pharmacology
- Cancer research
- Breast cancer
- Good health and well-being