NCIt definition : A water soluble, orally bioavailable inhibitor of the serine/threonine protein kinase
Akt (protein kinase B) and extracellular signal-regulated kinase (ERK), with potential
antineoplastic activity. Upon administration, dordaviprone binds to and inhibits the
activity of Akt and ERK, which may result in inhibition of the phosphatidylinositol
3-kinase (PI3K)/Akt signal transduction pathway as well as the mitogen-activated protein
kinase (MAPK)/ERK-mediated pathway. This may lead to the induction of tumor cell apoptosis
mediated by tumor necrosis factor (TNF)-related apoptosis-inducing ligand (TRAIL)/TRAIL
death receptor type 5 (DR5) signaling in AKT/ERK-overexpressing tumor cells. The PI3K/Akt
signaling pathway and MAPK/ERK pathway are upregulated in a variety of tumor cell
types and play a key role in tumor cell proliferation, differentiation and survival
by inhibiting apoptosis. In addition, ONC201 is able to cross the blood-brain barrier.;
Semantic type(s)