Preferred Label : KRAS G12D Degrader PT0253;
NCIt synonyms : KRAS G12D PROTAC Degrader PT0253; KRAS G12D PROTAC Protein Degrader PT0253; KRAS G12D Protein Degradation Agent PT0253; KRAS G12D Inhibitor PT0253; KRAS G12D Proteolysis Targeting Chimera Protein Degrader PT0253;
NCIt related terms : KRAS G12D Degrader ASP4396;
NCIt definition : A targeted degrader composed of an E3 ubiquitin ligase-binding moiety that is conjugated,
via a linker, to the oncogenic KRAS substitution mutation G12D-binding moiety, using
the proteolysis targeting chimera (PROTAC) technology, with potential antineoplastic
activity. Upon administration of KRAS G12D degrader PT0253, the KRAS G12D-targeting
moiety specifically targets and binds to the KRAS G12D mutated protein and the E3
ligase-binding moiety targets and binds to the E3 ubiquitin ligase, thereby forming
a ternary complex. This induces E3 ligase ubiquitination and proteasome-mediated degradation
of KRAS G12D. This prevents KRAS G12D-mediated signaling and activation of downstream
survival pathways. This leads to an inhibition of the growth of tumor cells that overexpress
KRAS G12D. KRAS, a member of the RAS family of oncogenes, serves an important role
in cell signaling, division and differentiation. Mutations of KRAS may induce constitutive
signal transduction leading to tumor cell proliferation, invasion, and metastasis.;
Molecule name : PT-0253;
Origin ID : C217663;
concept_is_in_subset
- has_target
