Preferred Label : MEK/Aurora Kinase Inhibitor BI 847325;
NCIt definition : An orally available dual inhibitor of mitogen-activated protein kinase kinase (MEK)
and Aurora kinases, with potential antineoplastic activity. Upon oral administration,
MEK/Aurora kinase inhibitor BI 847325 selectively binds to and inhibits the activity
of MEK, which both prevents the activation of MEK-dependent effector proteins and
inhibits growth factor-mediated cell signaling. BI 847325 also binds to and inhibits
the activity of the Aurora kinases A, B and C which may disrupt the assembly of the
mitotic spindle apparatus, prevent chromosome segregation, and inhibit both cellular
division and proliferation in Aurora kinase-overexpressing tumor cells. Altogether,
this leads to the inhibition of cell proliferation and tumor growth as well as the
induction of tumor regression. MEK, a dual-specificity threonine/tyrosine kinase that
plays a key role in the activation of the RAS/RAF/MEK/ERK signaling pathway, is frequently
upregulated in a variety of tumor cell types. Aurora kinases are serine-threonine
kinases that play essential roles in mitotic checkpoint control and are overexpressed
by a wide variety of cancer cell types.;
Molecule name : BI 847325;
Origin ID : C106126;
UMLS CUI : C3827151;
Semantic type(s)
- UMLS correspondences (same concept)
- concept_is_in_subset
