NCIt definition : An orally bioavailable inhibitor of both the serine/threonine protein kinase Aurora
kinase and FMS-related tyrosine kinase 3 (FLT3; STK1; CD135; FLK2), with potential
antineoplastic activity. Upon oral administration, Aurora kinase/FLT3 inhibitor EP0042
specifically binds to and inhibits Aurora kinase and FLT3, which interferes with the
activation of Aurora kinase- and FLT3-mediated signal transduction pathways. This
may result in the disruption of the assembly of the mitotic spindle apparatus, the
disruption of chromosome segregation and the inhibition of cell proliferation in tumor
cells that overexpress Aurora kinase and/or FLT3. Aurora kinase plays essential roles
in mitotic checkpoint control during mitosis. Aurora kinase and FLT3 are overexpressed
in a variety of cancers and play key roles in tumor cell proliferation.;
Semantic type(s)