Preferred Label : Padnarsertib;
NCIt synonyms : PAK4/NAMPT Inhibitor KPT-9274; PAK4/NAMPT Inhibitor ATG-019;
NCIt definition : An orally bioavailable inhibitor of both the serine/threonine kinase P21-activated
kinase 4 (PAK4) and the nicotinamide adenine dinucleotide (NAD)-synthesizing enzyme
nicotinamide phosphoribosyltransferase (NAMPT; NAMPRTase), with potential antineoplastic
activity. Upon administration, padnarsertib allosterically binds to, destabilizes
and causes degradation of PAK4. This inhibits PAK4-mediated signaling, induces cell
death in, and inhibits the proliferation of PAK4-overexpressing tumor cells. In addition,
padnarsertib binds to and inhibits the activity of NAMPT. This depletes cellular NAD
and inhibits NAD-dependent enzymes, both of which are needed for rapid cell proliferation;
this results in tumor cell death in NAMPT-overexpressing cancer cells. PAK4, a serine/threonine
kinase and member of the PAK family of proteins upregulated in various cancer cell
types, regulates cell motility, proliferation and survival. NAMPT, an enzyme that
is responsible for maintaining the intracellular NAD pool, plays a key role in the
regulation of cellular metabolism and has cytokine-like activities. NAMPT is often
overexpressed in a variety of cancers and metabolic disorders and tumor cells rely
on NAMPT activity for their NAD supply.;
UNII : 9T56TV18X7;
CAS number : 1643913-93-2;
Molecule name : KPT-9274; KCP-9274; ATG-019; ATG 019;
NCI Metathesaurus CUI : CL503763;
Origin ID : C126646;
UMLS CUI : C5706625;
Semantic type(s)
- UMLS correspondences (same concept)
- concept_is_in_subset
- has_target
