NCIt definition : An MDM2 (human homolog of murine double minute-2; HDM2) antagonist with potential
antineoplastic activity. Upon intravenous administration, RO6839921 binds to MDM2
and prevents the binding of the MDM2 protein to the transcriptional activation domain
of the tumor suppressor protein p53. By preventing MDM2-p53 interaction, the proteasome-mediated
enzymatic degradation of p53 is inhibited and the transcriptional activity of p53
is restored. This may result in the restoration of p53 signaling, followed by p53-mediated
induction of tumor cell apoptosis. MDM2, a zinc finger protein, is a negative regulator
of the p53 pathway and is often overexpressed in cancer cells; p53 inhibition has
been implicated in cancer cell proliferation and survival.;