Synonyms: BWA522 | compound 28 [PMID: 37556600]
Compound class:
Synthetic organic
Comment: BWA-522 is an orally active cereblon-targeting PROTAC degrader of the androgen receptor (AR) [2]. It was designed for potential to treat advanced prostate cancer. BWA-522 binds to the N-terminal domain (NTD) of the AR using a warhead derived from the antagonist EPI-002 (ralaniten) [1]. Exploiting the NTD is proposed as a strategy to target both wild type ARs and mutated ARs that have no ligand-binding domain (LBD) and that are therefore unsusceptible to androgen-competitive antagonist drugs.
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Bioactivity Comments |
BWA-522 efficiently degrades full-length AR (AR-FL) and AR with no LBD (AR-V7) in vitro [2]. |