Article
Small-molecule inhibitors of ERK-mediated immediate early gene expression and proliferation of melanoma cells expressing mutated BRaf.
The Biochemical journal - 1 May 2015
Samadani Ramin, Zhang Jun, Brophy Amanda, Oashi Taiji, Priyakumar U Deva, Raman E Prabhu, St John Franz J, Jung Kwan-Young, Fletcher Steven, Pozharski Edwin, MacKerell Alexander D, Shapiro Paul
Abstract excerpt
Constitutive activation of the extracellular-signal-regulated kinases 1 and 2 (ERK1/2) are central to regulating the proliferation and survival of many cancer cells. The current inhibitors of ERK1/2 target ATP binding or the catalytic site and are therefore limited in their utility for elucidating the complex biological roles of ERK1/2 through its phosphorylation and regulation of over 100 substrate proteins. To...
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