Preferred Label : Androgen Receptor Degrader HP518;
NCIt synonyms : Androgen Receptor Proteolysis Targeting Chimera Protein Degrader HP518; AR PROTAC Protein Degrader HP518; AR Degrader HP518;
NCIt definition : An orally available androgen receptor (AR)-targeted protein degrader, using the proteolysis
targeting chimera (PROTAC) technology, with potential antineoplastic activity. HP518
is composed of an AR ligand attached to an E3 ligase recognition moiety. Upon oral
administration of AR degrader HP518, the AR-binding moiety specifically targets and
binds to AR, particularly AR with AR ligand-binding domain (LBD) mutations. E3 ligase
is recruited to the AR by the E3 ligase recognition moiety and the AR target protein
is tagged by ubiquitin. This causes ubiquitination and degradation of AR by the proteasome.
This prevents the expression of AR target genes and halts AR-mediated signaling. This
results in an inhibition of proliferation in AR-overexpressing tumor cells. AR, a
hormone-regulated transcription factor, plays a key role in tumor cell proliferation
in castration-resistant prostate cancer (CRPC).;
Molecule name : HP 518; HP-518;
NCI Metathesaurus CUI : CL1926983;
Origin ID : C204801;
UMLS CUI : C5908058;
Semantic type(s)
- concept_is_in_subset
- has_target
