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
… to the effective inhibition of tumor growth in mice … degrader for the treatment of prostate
cancer and provides insights and guidance into the design of orally active PROTAC degraders. …

[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
… therapy for prostate cancerdegradation via Proteolysis Targeting Chimeras (PROTACs)
will be a better therapeutic strategy for targeting androgen receptor signaling in prostate cancer

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
… target for the treatment of prostate cancer. We report herein the design… chimeras (PROTAC)
androgen receptor (AR) degraders, such as compound A031. It could induce the degradation

Proteolysis-targeting chimera (PROTAC) for targeted protein degradation and cancer therapy

X Li, Y Song - Journal of hematology & oncology, 2020 - Springer
… This article reviews PROTAC-mediated degradation of critical oncoproteins in cancer, …
BRD4 degradation in HEK293T cells and reduced the viability of prostate carcinoma 22Rv1 …

Discovery of ARD-69 as a highly potent proteolysis targeting chimera (PROTAC) degrader of androgen receptor (AR) for the treatment of prostate cancer

X Han, C Wang, C Qin, W Xiang… - Journal of medicinal …, 2019 - ACS Publications
degraders of androgen receptor (AR), as exemplified by compound 34 (ARD-69). ARD-69
induces degradation of AR protein in AR-positive prostate cancer … AR+ prostate cancer cell …

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
… ) degrader, a series of novel proteolysis targeting chimeras (… evaluated for their AR degradation
activity against LNCaP (AR… affinity (85%) and degradation activity against AR. Due to the …

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
… therapeutic target to block AR signaling in prostate cancer cells. We demonstrated that
utilizing PROTAC for induced AR protein degradation via NTD represents an efficient alternative …

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

X Han, L Zhao, W Xiang, B Miao, C Qin… - Journal of Medicinal …, 2023 - ACS Publications
… -targeting chimera degrader. ARD-… degradation in both the LNCaP and VCaP prostate
cancer cell lines, potently and effectively suppresses AR-regulated genes, and inhibits cancer cell …

Protein degraders enter the clinic—a new approach to cancer therapy

D Chirnomas, KR Hornberger, CM Crews - Nature Reviews Clinical …, 2023 - nature.com
… for protein degraders that target the androgen receptor, the oestrogen receptor and BTK
have shown encouraging clinical activity in patients with prostate cancer, breast cancer and …

[HTML][HTML] Discovery of a peptide proteolysis-targeting chimera (PROTAC) drug of p300 for prostate cancer therapy

D Zhang, B Ma, D Liu, W Wu, T Zhou, Y Gao, C Yang… - …, 2024 - thelancet.com
… PROTAC drug demonstrated effective p300 degradation and cancer cell-killing capabilities
in … models, the p300 PROTAC drug showed potent p300 degradation and tumor suppression. …