Strategies toward discovery of potent and orally bioavailable proteolysis targeting chimera degraders of androgen receptor for the treatment of prostate cancer
Proteolysis targeting chimera (PROTAC) small-molecule degraders have emerged as a
promising new type of therapeutic agents, but the design of PROTAC degraders with …
promising new type of therapeutic agents, but the design of PROTAC degraders with …
Design and characterization of cereblon-mediated androgen receptor proteolysis-targeting chimeras
AD Takwale, SH Jo, YU Jeon, HS Kim, CH Shin… - European Journal of …, 2020 - Elsevier
Abstract Proteolysis-targeting chimera (PROTAC)-mediated protein degradation is a rapidly
emerging therapeutic intervention that induces the degradation of targeted proteins. Herein …
emerging therapeutic intervention that induces the degradation of targeted proteins. Herein …
Discovery of ARD-2051 as a potent and orally efficacious proteolysis targeting chimera (PROTAC) degrader of androgen receptor for the treatment of advanced …
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 …
(AR) proteolysis-targeting chimera degrader. ARD-2051 achieves DC50 values of 0.6 nM …
Discovery of ARD-69 as a highly potent proteolysis targeting chimera (PROTAC) degrader of androgen receptor (AR) for the treatment of prostate cancer
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 …
(AR), as exemplified by compound 34 (ARD-69). ARD-69 induces degradation of AR protein …
Discovery of A031 as effective proteolysis targeting chimera (PROTAC) androgen receptor (AR) degrader for the treatment of prostate cancer
L Chen, L Han, S Mao, P Xu, X Xu, R Zhao, Z Wu… - European Journal of …, 2021 - Elsevier
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 …
We report herein the design, synthesis, and biological evaluation of highly effective …
A comprehensive overview of small-molecule androgen receptor degraders: Recent progress and future perspectives
S Ha, G Luo, H Xiang - Journal of medicinal chemistry, 2022 - ACS Publications
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 …
proven to depend on the aberrant activation of androgen receptor (AR) signaling. Long-term …
Proteolysis targeting chimera (PROTAC) in drug discovery paradigm: Recent progress and future challenges
S Zeng, W Huang, X Zheng, Z Zhang, J Wang… - European journal of …, 2021 - Elsevier
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 …
ligase for target degradation via the ubiquitin-proteasome pathway, is a novel drug …
Discovery of highly potent and efficient PROTAC degraders of androgen receptor (AR) by employing weak binding affinity VHL E3 ligase ligands
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 …
castration-resistant prostate cancer (mCRPC). We report herein our design, synthesis, and …
A platform for the rapid synthesis of proteolysis targeting chimeras (Rapid-TAC) under miniaturized conditions
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 …
targeted protein degradation. PROTACs are composed of target protein ligand, E3 ligase …
[HTML][HTML] Degradation of proteins by PROTACs and other strategies
Y Wang, X Jiang, F Feng, W Liu, H Sun - Acta Pharmaceutica Sinica B, 2020 - Elsevier
Blocking the biological functions of scaffold proteins and aggregated proteins is a
challenging goal. PROTAC proteolysis-targeting chimaera (PROTAC) technology may be …
challenging goal. PROTAC proteolysis-targeting chimaera (PROTAC) technology may be …