NCIt definition : An orally available spiro-oxindole HDM2 (human double minute 2) antagonist with potential
antineoplastic activity. Upon oral administration, the p53-HDM2 protein-protein interaction
inhibitor MI-773 binds to HDM2, preventing the binding of the HDM2 protein to the
transcriptional activation domain of the tumor suppressor protein p53. By preventing
this HDM2-p53 interaction, the proteasome-mediated enzymatic degradation of p53 is
inhibited and the transcriptional activity of p53 is restored, which may result in
the restoration of p53 signaling and lead to the p53-mediated induction of tumor cell
apoptosis. HDM2, a zinc finger protein and a negative regulator of the p53 pathway,
is often overexpressed in cancer cells. It has been implicated in cancer cell proliferation
and survival.;
Semantic type(s)