Preferred Label : MEK1/2 Inhibitor PAS-004;
NCIt definition : An orally bioavailable macrocyclic inhibitor of mitogen-activated protein kinase kinase
(MAP2K, MAPK/ERK kinase, or MEK) 1 and 2, with potential antineoplastic activity.
Upon oral administration, MEK1/2 inhibitor PAS-004 selectively and allosterically
binds to and inhibits the activity of MEK1 and MEK2, preventing the activation of
MEK1/2-dependent effector proteins and transcription factors, which may result in
the inhibition of growth factor-mediated cell signaling and tumor cell proliferation.
MEK1/2 are dual-specificity threonine/tyrosine kinases that play key roles in the
activation of the RAS/RAF/MEK/ERK pathway that regulates cell growth. This pathway
is often dysregulated in a variety of tumor cell types through BRAF, KRAS and NRAS
mutations.;
Molecule name : PAS-004; PAS 004;
Origin ID : C209766;
concept_is_in_subset
- has_target
