RAF Inhibitors: Quantifying Drug-Target Occupancy at Active RAS-RAF Complexes in Live Cells

Mitogen-activated protein kinases (MAPKs) are a large family of proteins that regulate diverse cellular functions in eukaryotes, including gene expression, proliferation, differentiation and apoptosis (1). MAPK signaling pathways typically include three sequentially activated kinases, and these pathways are triggered in response to extracellular stimuli, such as cytokines, mitogens, growth factors and oxidative stress (1). Ultimately, the signal is transmitted to the nucleus, with the activation of a specific transcription factor that modulates the expression of one or more genes.

Among MAPK pathways, the RAS-RAF-MEK-ERK signaling pathway has been studied extensively. Mutations in RAS family proteins and resultant dysregulation of the signaling pathway are implicated in a variety of cancers. Therefore, this pathway is a popular target for anticancer drug development.

An overview of the RAS-RAF-MEK-ERK signaling pathway.
Continue reading “RAF Inhibitors: Quantifying Drug-Target Occupancy at Active RAS-RAF Complexes in Live Cells”

The Making of a Science App — Or — Things Your Professors Never Told You Scientists Do

For the past five months, I have been the outside observer to the conception, gestation and birth of a scientific app for the iPad®, the new Interactive Cell Signaling Pathways Tool that is now part 6 of the Promega iPad® App.

This all-new interactive cell signaling pathways module (iPad only) has been added to the Promega App. It allows readers to explore two pathways: MAPK/ERK and PI3K/mTOR. Aside from the coolness factor, the app gives users links to online resources, peer-reviewed literature and available products to aid in cell signaling research.

You see, my cube neighbor and fellow blogger, Michele, is one of the driving forces behind this App. Continue reading “The Making of a Science App — Or — Things Your Professors Never Told You Scientists Do”