Combination targets: some drugs may work best when they work together
... with a lack of oxygen, a state called hypoxia, they report. AZD6244 is a small molecule inhibitor developed by AstraZeneca to bind to and inhibit mek1 and MEK2 proteins, which together form a critical point on the pathway that controls the ongoing survival of cells. Defects along the pathway can lead...New Data for XL880, XL647 and XL184 to Be Presented at AACR-NCI-EORTC
...f cytotoxic therapy by XL844, an orally bioavailable inhibitor of Chk1 and Chk2 (Abstract #B228) -- XL518, a Potent Selective Orally Bioavailable mek1 Inhibitor, Downregulates the RAS/RAF/MEK/ERK Pathway In Vivo, Resulting in Tumor Growth Inhibition and Regression in Pre-Clinical Models (Abst...New Fusion Trans-Activator Plasmids for Studying Signal Transduction Pathways
...ctivates the GAL4-c-Fos fusion protein expressed from the pFA-cFos plasmid. The mechanism of this activation is not yet characterized. PKA, mek1 and other extracellular stimuli failed to activate the GAL4-c-Fos fusion protein (data not shown). ...Improved Vectors for PathDetect Trans-Reporting Systems
...smids with either the pFC-dbd or pFC2-dbd plasmids yielded similar background levels of luciferase activity. Since the mek1 protein is a known upstream activator of the Elk1 protein, the pFC-MEK1 plasmid was used to compare the activity of the pFA-Elk1 and ...In Vivo Signal Transduction Pathway Reporting Systems
...lk1 is phosphorylated and activated by MAPK. 10,11 The MEKK and mek1 proteins are both known activators of the Elk1 protein. Cotransf... of luciferase. These data are consistent with reports that both mek1 and MEKK proteins are known activators of the MAPK pathway. 16-...Yeast Protein Production System Features High Yields and One-Step Purification
...s, including the rat c-Jun N-terminal kinase (JNK) and the human mek1 gene products ( figure 4 ). Yield for these proteins ...K1 fusion protein. The GST tag was efficiently detached from the mek1 moiety by digesting the purified GST-MEK1 fusion protein with en...Production of Full-Length, Biologically Active MEK1WT and MEK1CA
...ressed and purified recombinant, wild-type human mek1 WT and a constitutively active mutant (MEK1 CA ) ...d in E. coli are significantly degraded. Wild-type mek1 WT can be used as a substrate for upstream MEK ... MEKK or mos. The uses for constitutively active mek1 CA include identifying potential substrates, ma...Assess the In Vivo Activation of Signal Transduction Pathways with PathDetect Reporting Systems
... In a similar fashion, the specificity of the pFA2-Elk1 fusion activator plasmid is demonstrated ( Figure 2 C). Since the mek1 protein is a known upstream activator of the Elk1 protein 12 the pFC-MEK1 plasmid, constitutively expressing this kinase, was u...