Mps1 is a dual specificity protein kinase that is essential for the bipolar attachment of chromosomes to the mitotic spindle and for maintaining the spindle assembly checkpoint until all chromosomes are properly attached. Mps1 is expressed at high levels during mitosis and is abundantly expressed in cancer cells. Disruption of Mps1 function induces… (More)
Activation of the transcription factor NF-kappaB has been linked to apoptosis, with the factor playing either an anti-apoptotic or a pro-apoptotic role, depending on the type of cell in which it is expressed.
Analysis of transcriptional activation properties of c-Jun chimeras in different cell lines suggests that it contains an activator domain (A1) that is negatively regulated by a cell type-specific inhibitor. A regulatory domain of c-Jun, delta, previously identified by in vitro experiments, also regulates transcriptional activation by c-Jun in vivo. The… (More)
Activation of the transcription factor NF-B has been linked to apoptosis, with the factor playing either an anti-apoptotic or a pro-apoptotic role, depending on the type of cell in which it is expressed. The transcription factor NF-B has for some years been recognized to be a central mediator of the gene expression induced in cells by pathogens or… (More)
A novel series of 4-arylaminoquinazolines were identified from a cell-based screening assay as potent apoptosis inducers. Through structure-activity relationship studies, MPC-6827 and its close structural analogue, MPI-0441138, were discovered as proapoptotic molecules and mitotic inhibitors with potencies at low nanomolar concentrations in multiple tumor… (More)
The AP-1 family of transcription factors, which includes the proto-oncogene products c-Jun and c-Fos, controls the stimulation of cellular genes by growth factors and the expression of oncogenes, including src and ras. Transcriptional activation by c-Jun is regulated by a cell-type-specific inhibitor that represses the activity of a transcriptional… (More)