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

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

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 …

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 …

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 …

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 …

Proteolysis targeting chimera (PROTAC), hijacking protein of interest (POI) and recruiting E3
ligase for target degradation via the ubiquitin-proteasome pathway, is a novel drug …

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 …

Proteolysis targeting chimera (PROTAC) is one of the most frequently used technologies for
targeted protein degradation. PROTACs are composed of target protein ligand, E3 ligase …

Blocking the biological functions of scaffold proteins and aggregated proteins is a
challenging goal. PROTAC proteolysis-targeting chimaera (PROTAC) technology may be …