A magic drug target: androgen receptor

D Li, W Zhou, J Pang, Q Tang, B Zhong… - Medicinal research …, 2019 - Wiley Online Library
Androgen receptor (AR) is closely associated with a group of hormone‐related diseases
including the cancers of prostate, breast, ovary, pancreas, etc and anabolic deficiencies …

TRIM24 is an oncogenic transcriptional activator in prostate cancer

AC Groner, L Cato, J de Tribolet-Hardy, T Bernasocchi… - Cancer cell, 2016 - cell.com
Androgen receptor (AR) signaling is a key driver of prostate cancer (PC). While androgen-
deprivation therapy is transiently effective in advanced disease, tumors often progress to a …

[HTML][HTML] ARv7 represses tumor-suppressor genes in castration-resistant prostate cancer

L Cato, J de Tribolet-Hardy, I Lee, JT Rottenberg… - Cancer cell, 2019 - cell.com
Androgen deprivation therapy for prostate cancer (PCa) benefits patients with early disease,
but becomes ineffective as PCa progresses to a castration-resistant state (CRPC). Initially …

Functional analysis of androgen receptor mutations that confer anti-androgen resistance identified in circulating cell-free DNA from prostate cancer patients

N Lallous, SV Volik, S Awrey, E Leblanc, R Tse… - Genome biology, 2016 - Springer
Background The androgen receptor (AR) is a pivotal drug target for the treatment of prostate
cancer, including its lethal castration-resistant (CRPC) form. All current non-steroidal AR …

[HTML][HTML] Therapy escape mechanisms in the malignant prostate

FR Santer, HHH Erb, RV McNeill - Seminars in cancer biology, 2015 - Elsevier
Androgen receptor (AR) is the main target for prostate cancer therapy. Clinical approaches
for AR inactivation include chemical castration, inhibition of androgen synthesis and AR …

Identification of a potent antiandrogen that targets the BF3 site of the androgen receptor and inhibits enzalutamide-resistant prostate cancer

RSN Munuganti, MDH Hassona, E Leblanc, K Frewin… - Chemistry & biology, 2014 - cell.com
There has been a resurgence of interest in the development of androgen receptor (AR)
inhibitors with alternative modes of action to overcome the development of resistance to …

Thio-2 Inhibits Key Signaling Pathways Required for the Development and Progression of Castration-resistant Prostate Cancer

A Neeb, I Figueiredo, D Bogdan, L Cato… - Molecular cancer …, 2024 - aacrjournals.org
Therapies that abrogate persistent androgen receptor (AR) signaling in castration-resistant
prostate cancer (CRPC) remain an unmet clinical need. The N-terminal domain of the AR …

Androgen receptor co-regulation in prostate cancer

D Senapati, S Kumari, HV Heemers - Asian Journal of Urology, 2020 - Elsevier
Prostate cancer (PCa) progression relies on androgen receptor (AR) action. Preventing AR's
ligand-activation is the frontline treatment for metastatic PCa. Androgen deprivation therapy …

[HTML][HTML] Allosteric small molecule modulators of nuclear receptors

FA Meijer, IA Leijten-van de Gevel… - Molecular and cellular …, 2019 - Elsevier
Abstract Nuclear Receptors (NRs) are multi-domain proteins, whose natural regulation
occurs via ligands for a classical, orthosteric, binding pocket and via intra-and inter-domain …

Selective modulation of the androgen receptor AF2 domain rescues degeneration in spinal bulbar muscular atrophy

NM Badders, A Korff, HC Miranda, PK Vuppala… - Nature medicine, 2018 - nature.com
Spinal bulbar muscular atrophy (SBMA) is a motor neuron disease caused by toxic gain of
function of the androgen receptor (AR). Previously, we found that co-regulator binding …