Preferred Label : Anti-HER2 GSPT1 Degrader ORM-5029;
NCIt synonyms : Antibody Neodegrader Conjugate ORM-5029; Anti-HER-2 GSPT1 Degrader ORM-5029; AnDC ORM-5029; Pertuzumab-SMol006 ORM-5029;
NCIt definition : A targeted protein degrader (TPD) composed of pertuzumab, an antibody directed against
the tumor-associated antigen (TAA) human tyrosine kinase receptor epidermal growth
factor receptor 2 (HER2; ErbB2; HER-2), conjugated, via a Val-Cit PABc cleavable linker,
to SMol006, a membrane-permeable selective molecular glue degrader (MGD) of the translational
termination factor GSPT1, with potential antineoplastic activity. Upon intravenous
administration, anti-HER2 GSPT1 degrader ORM-5029 specifically targets and binds,
with its pertuzumab moiety, to HER-2-expressing tumor cells. Upon internalization
and cleavage, SMol006 specifically targets and binds to GSPT1, leading to GSPT1 degradation
via the E3 ubiquitin ligase pathway. This disrupts oncogenic signaling, inhibits proliferation,
and induces apoptosis in HER-2-driven tumors. The translation termination factor GSPT1,
a G-loop degron-containing protein, plays a key role in protein translation and is
dysregulated in various tumor cell types.;
Molecule name : ORM-5029; ORM 5029;
NCI Metathesaurus CUI : CL1905250;
Origin ID : C191715;
UMLS CUI : C5787256;
Semantic type(s)
- concept_is_in_subset
- has_target
