The androgen receptor, androgen synthesis, and new designer antiandrogens for metastatic castration-resistant prostate cancer: teaching old dogs new tricks

R Lieberman - American Journal of Therapeutics, 2013 - journals.lww.com
Until recently, the only systemic regimen known to impact overall survival (OS) in men with
symptomatic metastatic castration-resistant prostate cancer (mCRPC) was a taxane-based …

Cross-resistance to abiraterone and enzalutamide in castration resistance prostate cancer cellular models is mediated by AR transcriptional reactivation

I Simon, S Perales, L Casado-Medina… - Cancers, 2021 - mdpi.com
Simple Summary Prostate cancer is the second most common cancer in males. In prostate
cancer cells, androgens bind and activate the intracellular mediator called Androgen …

Treatment of castration-resistant prostate cancer: updates on therapeutics targeting the androgen receptor signaling pathway

W Zhu, DS Zhu, RA Madan, JL Gulley… - American journal of …, 2010 - journals.lww.com
Androgens play a critical role in the progression of castration-resistant prostate cancer
through androgen receptor (AR)-regulated signaling pathways. Progress has been made in …

[HTML][HTML] Novel non-AR therapeutic targets in castrate resistant prostate cancer

PJ Toren, ME Gleave - Translational Andrology and Urology, 2013 - ncbi.nlm.nih.gov
Castrate resistant prostate cancer (CRPC) remains a disease with significant morbidity and
mortality. The recent approval of abiraterone and enzalutamide highlight the improvements …

Androgen receptor functions in castration-resistant prostate cancer and mechanisms of resistance to new agents targeting the androgen axis

X Yuan, C Cai, S Chen, Z Yu, SP Balk - Oncogene, 2014 - nature.com
The metabolic functions of androgen receptor (AR) in normal prostate are circumvented in
prostate cancer (PCa) to drive tumor growth, and the AR also can acquire new growth …

Targeting constitutively active androgen receptor splice variants in castration resistant prostate cancer

MT Schweizer, SR Plymate - Expert opinion on therapeutic targets, 2016 - Taylor & Francis
In the castration-resistant state, androgen receptor (AR)-signaling remains a critical driver of
prostate cancer cell growth. This realization led to the development of the next-generation …

A profile of enzalutamide for the treatment of advanced castration resistant prostate cancer

R Greasley, M Khabazhaitajer… - Cancer Management and …, 2015 - Taylor & Francis
Recent advances in understanding the mechanisms underlying the development and
progression of castration resistant prostate cancer from androgen-sensitive prostate cancer …

Battling resistance mechanisms in antihormonal prostate cancer treatment: Novel agents and combinations

DJ De Maeseneer, C Van Praet, N Lumen… - … Oncology: Seminars and …, 2015 - Elsevier
Prostate cancer (PCa) is a hormone-sensitive disease. Androgen deprivation therapy lowers
serum testosterone levels (castration) or blocks the androgen receptor (AR) ligand-binding …

Galeterone prevents androgen receptor binding to chromatin and enhances degradation of mutant androgen receptor

Z Yu, C Cai, S Gao, NI Simon, HC Shen, SP Balk - Clinical cancer research, 2014 - AACR
Purpose: Galeterone inhibits the enzyme CYP17A1 and is currently in phase II clinical trials
for castration-resistant prostate cancer (CRPC). Galeterone is also a direct androgen …

Enzalutamide and blocking androgen receptor in advanced prostate cancer: lessons learnt from the history of drug development of antiandrogens

Y Ito, MD Sadar - Research and Reports in Urology, 2018 - Taylor & Francis
Enzalutamide is a nonsteroidal antiandrogen for the treatment of metastatic castration-
resistant prostate cancer (mCRPC) both before and after chemotherapy. Enzalutamide is …