Synonyms: compound 11 [PMID: 31804827]
Compound class:
Synthetic organic
Comment: ARD-266 is a potent proteolysis-targeting chimera (PROTAC) degrader of the androgen receptor (AR) [1]. Its design highlights that using an E3 ligase ligand with low affinity (Ki of 2-3 μM) in a PROTAC can still achieve a very potent degrading effect against the AR. Ubiquitination and proteasomal degradation is mediated by the compound's ligand that binds to the VHL constituent of the VHL/cullin2 E3 ligase complex. The AR antagonist component of ARD-266 is the same as that utilised in the previously reported AR degrader, ARD-69.
|
|
Bioactivity Comments |
ARD-266 potently promotes degradation of the AR (DC50 values of 0.2-1 nM) and decreases AR protein level by >95% (at 100 nM) in AR+ve prostate cancer cell lines [1]. |
Selectivity at nuclear hormone receptors | ||||||||||||||||||||||||||||||||||
Key to terms and symbols | Click column headers to sort | |||||||||||||||||||||||||||||||||
|