Preferred Label : Vepdegestrant;
NCIt synonyms : PROTAC Protein Degrader ARV-471; ER alpha PROTAC Protein Degrader ARV-471; Estrogen Receptor alpha PROTAC Protein Degrader ARV-471; 2,6-Piperidinedione, 3-(1,3-dihydro-1-oxo-5-(4-((1-(4-((1R,2S)-1,2,3,4-tetrahydro-6-hydroxy-2-phenyl-1-naphthalenyl)phenyl)-4-piperidinyl)methyl)-1-piperazinyl)-2H-isoindol-2-yl)-,
(3S)-; ER alpha Proteolysis-targeting Chimera Protein Degrader ARV-471;
NCIt definition : An orally available hetero-bifunctional molecule and selective estrogen receptor (ER)
alpha-targeted protein degrader, using the proteolysis targeting chimera (PROTAC)
technology, with potential antineoplastic activity. Vepdegestrant is composed of an
ER alpha ligand attached to an E3 ligase recognition moiety. Upon oral administration,vepdegestrant
targets and binds to the ER ligand binding domain on ER alpha. E3 ligase is recruited
to the ER by the E3 ligase recognition moiety and ER alpha is tagged by ubiquitin.
This causes ubiquitination and degradation of ER alpha by the proteasome. This decreases
ER alpha protein levels, decreases the expression of ER alpha-target genes and halts
ER-mediated signaling. This results in an inhibition of proliferation in ER alpha-overexpressing
tumor cells. In addition, the degradation of the ER alpha protein releases the ARV-471
and can bind to additional ER alpha target proteins. ER alpha is overexpressed in
a variety of cancers and plays a key role in cancer cell proliferation.;
UNII : WC1U3R1YMI;
CAS number : 2229711-68-4; a href https://gsrs.ncats.nih.gov/ginas/app/beta/browse-substance?search 2229711-68-4
alt lien vers site G-SRS target _blank img src /img/logos/logo_g-srs.png alt Logo
G-SRS /a ;
Molecule name : ARV 471; ARV-471; PF-07850327; PF 07850327;
NCI Metathesaurus CUI : CL978634;
Origin ID : C165420;
UMLS CUI : C5706575;
Semantic type(s)
- concept_is_in_subset
- has_target
