Preferred Label : BCL6 Degrader BMS-986458;
NCIt synonyms : BCL6 LDD BMS-986458; Ligand Directed Degrader BMS-986458;
NCIt definition : An orally bioavailable ligand directed degrader (LDD) 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, with potential antineoplastic activity. Upon oral administration,
BCL6 degrader BMS-986458 specifically and simultaneously targets and binds to BCL6
on tumor cells and 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, overexpressed
in certain tumor cells, serves an important role in cell signaling and tumor cell
proliferation.;
Molecule name : BMS-986458; BMS 986458;
NCI Metathesaurus CUI : CL1921199;
Origin ID : C202207;
UMLS CUI : C5907945;
Semantic type(s)
- concept_is_in_subset
- has_target
