Preferred Label : Mutant p53 Activator COTI-2;
NCIt related terms : COTI-2;
NCIt definition : An orally available third generation thiosemicarbazone and activator of mutant forms
of the p53 protein, with potential antineoplastic activity. Upon oral administration,
mutant p53 activator COTI-2 targets and binds to the misfolded mutant forms of the
p53 protein, which induces a conformational change that normalizes p53 and restores
its activity. This induces apoptosis in tumor cells in which the p53 protein is mutated.
In addition, COTI-2 inhibits the activation of Akt2 and prevents the activation of
the PI3K/AKT/mTOR pathway, thereby inducing apoptosis in cancer cells in which this
pathway is overexpressed. p53, a tumor suppressor protein, plays a key role in controlling
cellular proliferation and survival. High levels of mutant p53 are seen in many cancers
and are associated with uncontrolled cellular growth.;
UNII : 2BTA1O65BR;
CAS number : 1039455-84-9;
Molecule name : Coti-2;
Origin ID : C121951;
UMLS CUI : C4053651;
Semantic type(s)
- concept_is_in_subset
- has_target
