Preferred Label : Anti-CD33 GSPT1 Degrader BMS-986497;
NCIt synonyms : Degrader-Antibody Conjugate BMS-986497; Targeted Protein Degrader BMS-986497; Anti-CD33 Antibody-enabled GSPT1 Degrader BMS-986497; TPD GSPT1 BMS-986497;
NCIt definition : A targeted protein degrader (TPD) composed of OR000283, an antibody directed against
the tumor-associated antigen (TAA) cluster of differentiation 33 (CD33), conjugated,
via a cleavable beta-glucuronide 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-CD33 GSPT1
degrader BMS-986497 specifically targets and binds, with its antibody moiety, to CD33-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 CD33-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. CD33, a cell surface antigen expressed on normal non-pluripotent hematopoietic
stem cells, is overexpressed on myeloid leukemia cells.;
Molecule name : ORM-6151; BMS 986497; ORM 6151; BMS-986497;
Origin ID : C207963;
concept_is_in_subset
- has_target
