Preferred Label : MDM2 Degrader KT-253;
NCIt definition : A small molecule protein and selective degrader of the oncoprotein murine double minute
2 (MDM2), with potential immunomodulating and antineoplastic activities. Upon administration,
MDM2 degrader KT-253 binds to MDM2 and the E3 (ubiquitin) ligase and targets MDM2
for ubiquitination. This induces proteasome-mediated degradation of MDM2 and prevents
its binding to the transcriptional activation domain of the tumor suppressor protein
p53. By preventing this MDM2-p53 interaction, the transcriptional activity of p53
is restored and leads to the stabilization of p53 levels. This leads to p53-mediated
induction of tumor cell apoptosis. MDM2, a zinc finger protein and a negative regulator
of the p53 pathway, is overexpressed in cancer cells; it plays a key role in cancer
cell proliferation and survival.;
Molecule name : KT-253; KT 253;
NCI Metathesaurus CUI : CL1907129;
Origin ID : C200323;
UMLS CUI : C5853560;
Semantic type(s)
- concept_is_in_subset
- has_target
