[HTML][HTML] A highly potent PROTAC androgen receptor (AR) degrader ARD-61 effectively inhibits AR-positive breast cancer cell growth in vitro and tumor growth in vivo

L Zhao, X Han, J Lu, D McEachern, S Wang - Neoplasia, 2020 - Elsevier
… in AR-positive (AR+) breast cancer. We have recently reported the discovery of a highly potent
PROTAC AR degrader, … Using metribolone (R1881), a highly potent AR agonist, we further …

Discovery of ARD-2051 as a potent and orally efficacious proteolysis targeting chimera (PROTAC) degrader of androgen receptor for the treatment of advanced …

X Han, L Zhao, W Xiang, B Miao, C Qin… - Journal of Medicinal …, 2023 - ACS Publications
… to the discovery of ARD-2051 as a highly potent and orally … previously employed AR ligand
6 for the design of a highly potent … that AR degradation induced by ARD-2051 is effectively

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
… A series of PROTAC AR degraders were synthesized using … that A031 was a potent AR
degrader. The tumor growth … design of highly potent and efficient PROTAC AR degraders. …

Discovery of ARD-2585 as an exceptionally potent and orally active PROTAC degrader of androgen receptor for the treatment of advanced prostate cancer

W Xiang, L Zhao, X Han, C Qin, B Miao… - Journal of medicinal …, 2021 - ACS Publications
… bioavailable PROTAC AR degraders, we decided to employ cereblon ligands. … fairly potent
and effective AR degrader and compound 13 is a highly potent and very effective AR degrader

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 …

W Xiang, L Zhao, X Han, T Xu, S Kregel… - Journal of Medicinal …, 2023 - ACS Publications
… of the androgen receptor (AR). ARD-1676 was designed … of potent and orally bioavailable
PROTAC AR degraders using a … is a highly potent and effective AR degrader but is slightly less …

Strategies toward discovery of potent and orally bioavailable proteolysis targeting chimera degraders of androgen receptor for the treatment of prostate cancer

X Han, L Zhao, W Xiang, C Qin, B Miao… - Journal of medicinal …, 2021 - ACS Publications
… the discovery of highly potent PROTAC degraders of androgenAR degraders is critical for
the potent and effective reduction of … These general strategies employed in our study provide …

Discovery of BWA-522, a first-in-class and orally bioavailable PROTAC degrader of the androgen receptor targeting N-terminal domain for the treatment of prostate …

B Zhang, C Liu, Z Yang, S Zhang, X Hu… - Journal of medicinal …, 2023 - ACS Publications
… improvement of degradation activity following employment of … are highly potent and effective
in reducing AR-FL and AR-V7 … potent PROTACs led to the identification of the most effective

The design, synthesis and anti-tumor mechanism study of new androgen receptor degrader

H Xie, JJ Liang, YL Wang, TX Hu, JY Wang… - European Journal of …, 2020 - Elsevier
… chimeras (PROTAC) was … using several different classes of AR antagonists and a von
Hippel−Lindau (VHL) ligand [9]. The most potent one exhibited excellent degradation potency

Design, synthesis, and characterization of PROTACs targeting the androgen receptor in prostate and lung cancer models

LM Gockel, V Pfeifer, F Baltes… - Archiv der …, 2022 - Wiley Online Library
recruiting cereblon, we were able to demonstrate the potent … [ 33 ] For our PROTAC design,
we contemplated CRBN as the most … the hypothesis that AR inhibition or degradation may not …

Designed, synthesized and biological evaluation of proteolysis targeting chimeras (PROTACs) as AR degraders for prostate cancer treatment

JJ Liang, H Xie, RH Yang, N Wang, ZJ Zheng… - Bioorganic & Medicinal …, 2021 - Elsevier
potent and potentially safe androgen receptor (AR) degrader, … of highly potent and effective
AR degraders are needed more … PROTAC conjugates are currently in progress in our group. …