ARD-69 is a PROTAC degrader that targets the androgen receptor (AR) through the E3 ubiquitin ligase VHL, facilitating AR protein degradation in AR-positive prostate cancer cells. By binding to both the AR ligand-binding domain and VHL, ARD-69 promotes the recruitment of AR to the E3 ubiquitin ligase complex, leading to proteasomal degradation and subsequent inhibition of AR signaling pathways, including AR-regulated gene expression such as PSA and TMPRSS2. ARD-69 is a valuable tool for studying mechanisms underlying castration-resistant prostate cancer (mCRPC). The compound consists of an AR antagonist, a specific PROTAC linker, and a VHL-type E3 ubiquitinase ligand.
ARD-69 is a PROTAC degrader that targets the androgen receptor (AR) through the E3 ubiquitin ligase VHL, facilitating AR protein degradation in AR-positive prostate cancer cells. By binding to both the AR ligand-binding domain and VHL, ARD-69 promotes the recruitment of AR to the E3 ubiquitin ligase complex, leading to proteasomal degradation and subsequent inhibition of AR signaling pathways, including AR-regulated gene expression such as PSA and TMPRSS2. ARD-69 is a valuable tool for studying mechanisms underlying castration-resistant prostate cancer (mCRPC). The compound consists of an AR antagonist, a specific PROTAC linker, and a VHL-type E3 ubiquitinase ligand.
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