Androgen receptor variant-driven prostate cancer: clinical implications and therapeutic targeting

ES Antonarakis, AJ Armstrong, SM Dehm… - Prostate cancer and …, 2016 - nature.com
While there are myriad mechanisms of primary and acquired resistance to conventional and
next-generation hormonal therapies in prostate cancer, the potential role of androgen …

[HTML][HTML] Non-genomic actions of the androgen receptor in prostate cancer

JK Leung, MD Sadar - Frontiers in endocrinology, 2017 - frontiersin.org
Androgen receptor (AR) is a validated drug target for prostate cancer based on its role in
proliferation, survival, and metastases of prostate cancer cells. Unfortunately, despite recent …

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
We report small molecular PROTAC compounds targeting the androgen receptor N-terminal
domain (AR-NTD), which were obtained by tethering AR-NTD antagonists and different …

Diverse AR-V7 cistromes in castration-resistant prostate cancer are governed by HoxB13

Z Chen, D Wu, JM Thomas-Ahner… - Proceedings of the …, 2018 - National Acad Sciences
The constitutively active androgen receptor (AR) splice variant 7 (AR-V7) plays an important
role in the progression of castration-resistant prostate cancer (CRPC). Although biomarker …

[HTML][HTML] Androgen receptor-dependent and-independent mechanisms driving prostate cancer progression: Opportunities for therapeutic targeting from multiple angles

DT Hoang, KA Iczkowski, D Kilari, W See… - Oncotarget, 2017 - ncbi.nlm.nih.gov
Despite aggressive treatment for localized cancer, prostate cancer (PC) remains a leading
cause of cancer-related death for American men due to a subset of patients progressing to …

[HTML][HTML] Molecular and cellular mechanisms of castration resistant prostate cancer

Y Huang, X Jiang, X Liang, G Jiang - Oncology letters, 2018 - spandidos-publications.com
With increases in the mortality rate and number of patients with prostate cancer (PCa), PCa,
particularly the advanced and metastatic disease, has been the focus of a number of studies …

Androgen receptor targeted therapies in castration‐resistant prostate cancer: bench to clinic

Y Imamura, MD Sadar - International Journal of Urology, 2016 - Wiley Online Library
The androgen receptor is a transcription factor and validated therapeutic target for prostate
cancer. Androgen deprivation therapy remains the gold standard treatment, but it is not …

Molecules targeting the androgen receptor (AR) signaling axis beyond the AR‐Ligand binding domain

NGRD Elshan, MB Rettig… - Medicinal research reviews, 2019 - Wiley Online Library
Prostate cancer (PCa) is the second most common cause of cancer‐related mortality in men
in the United States. The androgen receptor (AR) and the physiological pathways it …

Targeting the N-terminal domain of the androgen receptor: The effective approach in therapy of CRPC

Y Ji, R Zhang, X Han, J Zhou - European Journal of Medicinal Chemistry, 2023 - Elsevier
The androgen receptor (AR) is dominant in prostate cancer (PCa) pathology. Current
therapeutic agents for advanced PCa include androgen synthesis inhibitors and AR …

[HTML][HTML] Natural product-based studies for the management of castration-resistant prostate cancer: Computational to clinical studies

RK Singla, P Sharma, AK Dubey… - Frontiers in …, 2021 - frontiersin.org
Background: With prostate cancer being the fifth-greatest cause of cancer mortality in 2020,
there is a dire need to expand the available treatment options. Castration-resistant prostate …