NCIt definition : An orally bioavailable, small molecule inhibitor of the nicotinamide adenine dinucleotide
(NAD)-synthesizing enzyme nicotinamide phosphoribosyltransferase (NAMPT; NAMPRTase),
with potential antineoplastic activity. Upon oral administration, NAMPT inhibitor
OT-82 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 cell death in NAMPT-overexpressing cancer cells. 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 overexpressed
in a variety of cancers and metabolic disorders; tumor cells rely on NAMPT activity
for their NAD supply.;
Semantic type(s)