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.
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References |
1. Han X, Zhao L, Xiang W, Qin C, Miao B, Xu T, Wang M, Yang CY, Chinnaswamy K, Stuckey J et al.. (2019)
Discovery of Highly Potent and Efficient PROTAC Degraders of Androgen Receptor (AR) by Employing Weak Binding Affinity VHL E3 Ligase Ligands. J Med Chem, 62 (24): 11218-11231. [PMID:31804827] |