Preferred Label : SMARCA2 Degrader PRT3789;
NCIt synonyms : SMARCA2 Protein Degrader PRT3789;
NCIt definition : A targeted protein degrader (TPD) of SWI/SNF-related matrix-associated actin-dependent
regulator of chromatin subfamily A member 2 (SMARCA2; BRM), with potential antineoplastic
activity. PRT3789 is comprised of an E3 ubiquitin ligase-binding moiety conjugated,
via a chemical linker, to a SMARCA2-binding moiety. Upon administration of SMARCA2
degrader PRT3789, the SMARCA2-binding moiety specifically targets and binds to SMARCA2
and the E3 ubiquitin 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 SMARCA2. This may lead to the inhibition of the SWI/SNF (BRG1/BRM-associated
factor; BAF) chromatin remodeling complex, disrupt chromatin remodeling and gene expression,
and result in the downregulation of oncogenic pathways and the inhibition of tumor
cell proliferation in SWI/SNF-related matrix-associated actin-dependent regulator
of chromatin subfamily A member 4 (SMARCA4; BRG1)-deleted cancers. SMARCA2 and SMARCA4
are the primary ATPase components and mutually exclusive core catalytic subunits of
the SWI/SNF chromatin remodeling complex, an important regulator of transcriptional
programs and gene expression. SMARCA4 expression is absent in certain cancer cells,
and these SMARCA4-deleted cancer cells depend on SMARCA2 for survival.;
Molecule name : PRT-3789; PRT 3789;
NCI Metathesaurus CUI : CL1905842;
Origin ID : C198690;
concept_is_in_subset
- has_target
