Preferred Label : Pan-RAF/MEK Molecular Glue NST-628;
NCIt definition : An orally bioavailable non-covalent non-degrading pan-RAF/mitogen-activated protein
kinase kinase (MAP2K, MAPK/ERK kinase, or MEK) dual molecular glue, with potential
antineoplastic activity. Upon oral administration, pan-RAF/MEK molecular glue NST-628
targets and glues A-RAF, B-RAF and C-RAF protein kinases with unphosphorylated MEK1,
forming a stable and inactive RAF-MEK complex. This prevents the phosphorylation and
activation of MEK by RAF, inhibits the activity of MEK, thereby preventing the activation
of MEK-dependent effector proteins and transcription factors, which may result in
the inhibition of growth factor-mediated cell signaling and tumor cell proliferation.
Oncogenic mutations in RAF plays a key role in the overactivation of the RAS-mitogen-activated
protein kinase (MAPK) pathway and drives tumor cell proliferation and survival. 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. NST-628 is
able to cross the blood-brain barrier (BBB).;
Molecule name : NST-628; NST 628;
Origin ID : C207813;
concept_is_in_subset
- has_target
