Article
Discovery of a novel ERK inhibitor with activity in models of acquired resistance to BRAF and MEK inhibitors.
Cancer discovery - 1 Jul 2013
Morris Erick J, Jha Sharda, Restaino Clifford R, Dayananth Priya, Zhu Hugh, Cooper Alan, Carr Donna, Deng Yongi, Jin Weihong, Black Stuart, Long Brian, Liu Jenny, Dinunzio Edward, Windsor William, Zhang Rumin, Zhao Shuxia, Angagaw Minilik H, Pinheiro Elaine M, Desai Jagdish, Xiao Li, Shipps Gerald, Hruza Alan, Wang James, Kelly Joe, Paliwal Sunil, Gao Xiaolei, Babu Boga Sobhana, Zhu Liang, Daublain Pierre, Zhang Ling, Lutterbach Bart A, Pelletier Marc R, Philippar Ulrike, Siliphaivanh Phieng, Witter David, Kirschmeier Paul, Bishop W Robert, Hicklin Daniel, Gilliland D Gary, Jayaraman Lata, Zawel Leigh, Fawell Stephen, Samatar Ahmed A
Abstract excerpt
The high frequency of activating RAS or BRAF mutations in cancer provides strong rationale for targeting the mitogen-activated protein kinase (MAPK) pathway. Selective BRAF and MAP-ERK kinase (MEK) inhibitors have shown clinical efficacy in patients with melanoma. However, the majority of responses are transient, and resistance is often associated with pathway reactivation of the extracellular signal-regulated...
Read the complete abstract on PubMedTopics
- Cell Line, Tumor
- Cell Proliferation