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 …
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 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 …
[HTML][HTML] Androgen receptor degradation by the proteolysis-targeting chimera ARCC-4 outperforms enzalutamide in cellular models of prostate cancer drug resistance
J Salami, S Alabi, RR Willard, NJ Vitale, J Wang… - Communications …, 2018 - nature.com
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 …
activity using competitive antagonists, such as enzalutamide remains a frontline therapy for …
Targeting androgen receptor and the variants by an orally bioavailable Proteolysis Targeting Chimeras compound in castration resistant prostate cancer
CL Hung, HH Liu, CW Fu, HH Yeh, TL Hu, ZK Kuo… - …, 2023 - thelancet.com
Background Despite the advent of improved therapeutic options for advanced prostate
cancer, the durability of clinical benefits is limited due to inevitable development of …
cancer, the durability of clinical benefits is limited due to inevitable development of …
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 …
Discovery of ARD-1676 as a highly potent and orally efficacious AR PROTAC degrader with a broad activity against AR mutants for the treatment of AR+ human …
We report herein the discovery and extensive characterization of ARD-1676, a highly potent
and orally efficacious PROTAC degrader of the androgen receptor (AR). ARD-1676 was …
and orally efficacious PROTAC degrader of the androgen receptor (AR). ARD-1676 was …