We report herein the discovery of highly potent PROTAC degraders of androgen receptor
(AR), as exemplified by compound 34 (ARD-69). ARD-69 induces degradation of AR protein …

We report the discovery of ARD-2051 as a potent and orally efficacious androgen receptor
(AR) proteolysis-targeting chimera degrader. ARD-2051 achieves DC50 values of 0.6 nM …

Androgen receptor (AR) is an effective therapeutic target for the treatment of prostate cancer.
We report herein the design, synthesis, and biological evaluation of highly effective …

Proteolysis targeting chimera (PROTAC) small-molecule degraders have emerged as a
promising new type of therapeutic agents, but the design of PROTAC degraders with …

Androgen receptor (AR) is a validated therapeutic target for the treatment of metastatic
castration-resistant prostate cancer (mCRPC). We report herein our design, synthesis, and …

Abstract Proteolysis-targeting chimera (PROTAC)-mediated protein degradation is a rapidly
emerging therapeutic intervention that induces the degradation of targeted proteins. Herein …

The androgen receptor is a major driver of prostate cancer and inhibition of its transcriptional
activity using competitive antagonists, such as enzalutamide remains a frontline therapy for …

Androgen receptor (AR) antagonists, such as enzalutamide, have had a major impact on the
treatment of metastatic castration-resistant prostate cancer (CRPC). However, even with the …

Background: The Androgen Receptor (AR) remains the principal driver of castrationresistant
prostate cancer during the transition from a localized to metastatic disease. Most patients …

Prostate cancer (PC), the second most prevalent malignancy in men worldwide, has been
proven to depend on the aberrant activation of androgen receptor (AR) signaling. Long-term …