Preferred Label : BCL6 Degrader ARV-393;
NCIt synonyms : Proteolysis-targeting Chimera Protein Degrader ARV-393; PROTAC BCL6 Degrader ARV-393;
NCIt definition : An orally bioavailable, targeted degrader composed of an E3 ubiquitin ligase-binding
moiety that is conjugated, via a linker, to a B-cell lymphoma 6 protein (BCL6; BCL-6)-binding
moiety using the proteolysis targeting chimera (PROTAC) technology, with potential
antineoplastic activity. Upon oral administration of BCL6 degrader ARV-393, the BCL6-binding
moiety specifically targets and binds to BCL6 on tumor cells while the E3 ubiquitin
ligase-binding moiety targets and binds to E3 ubiquitin ligase, thereby creating a
ternary complex. This induces E3 ligase ubiquitination and proteasome-mediated degradation
of BCL6. This prevents BCL6-mediated signaling and activation of downstream survival
pathways. This leads to an inhibition of the growth of tumor cells that overexpress
BCL6. BCL6, a transcriptional repressor overexpressed in certain tumor cells, serves
an important role in cell signaling and tumor cell proliferation.;
Molecule name : ARV-393; ARV 393;
Origin ID : C209867;
concept_is_in_subset
- has_target
