Nuclear receptors: recent drug discovery for cancer therapies

L Zhao, S Zhou, JÅ Gustafsson - Endocrine reviews, 2019 - academic.oup.com
Nuclear receptors (NRs) are transcription factors actively involved in many aspects of human
physiology and pathology, serving as sensors of stimuli, master regulators of downstream …

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 …

Discovery and development of Galeterone (TOK-001 or VN/124-1) for the treatment of all stages of prostate cancer

VCO Njar, AMH Brodie - 2015 - ACS Publications
In our effort to discover potent and specific inhibitors of 17α-hydroxylase/17, 20-lyase
(CYP17), the key enzyme which catalyzes the biosynthesis of androgens from progestins, 3β …

[HTML][HTML] Galeterone and VNPT55 induce proteasomal degradation of AR/AR-V7, induce significant apoptosis via cytochrome c release and suppress growth of …

AK Kwegyir-Afful, S Ramalingam… - Oncotarget, 2015 - ncbi.nlm.nih.gov
Galeterone (Gal) is a first-in-class multi-target oral small molecule that will soon enter pivotal
phase III clinical trials in castration resistant prostate cancer (CRPC) patients. Gal disrupts …

Androgen receptor modulation optimized for response (ARMOR) phase I and II studies: galeterone for the treatment of castration-resistant prostate cancer

B Montgomery, MA Eisenberger, MB Rettig, F Chu… - Clinical Cancer …, 2016 - AACR
Purpose: Galeterone is a selective, multitargeted agent that inhibits CYP17, antagonizes the
androgen receptor (AR), and reduces AR expression in prostate cancer cells by causing an …

Androgen receptor signaling inhibition in advanced castration resistance prostate cancer: what is expected for the near future?

J Pozas, S Álvarez Rodríguez, VA Fernández, J Burgos… - Cancers, 2022 - mdpi.com
Simple Summary Prostate cancer progression is mainly driven by the androgen receptor
(AR) signaling pathway and its inhibition has been the cornerstone in the treatment of …

Galeterone for the treatment of advanced prostate cancer: the evidence to date

DA Bastos, ES Antonarakis - Drug design, development and …, 2016 - Taylor & Francis
Major advances have been achieved recently in the treatment of metastatic castration-
resistant prostate cancer, resulting in significant improvements in quality of life and survival …

SiNVICT: ultra-sensitive detection of single nucleotide variants and indels in circulating tumour DNA

C Kockan, F Hach, I Sarrafi, RH Bell… - …, 2017 - academic.oup.com
Motivation Successful development and application of precision oncology approaches
require robust elucidation of the genomic landscape of a patient's cancer and, ideally, the …

Targeting androgen receptor versus targeting androgens to suppress castration resistant prostate cancer

C Guo, S Yeh, Y Niu, G Li, J Zheng, L Li, C Chang - Cancer letters, 2017 - Elsevier
Prostate cancer (PCa) is the 2nd leading cause of cancer-related death among men in the
United States and its progression is tightly associated with the androgen/androgen receptor …

Phase I and II therapies targeting the androgen receptor for the treatment of castration resistant prostate cancer

A Dellis, AG Papatsoris - Expert opinion on investigational drugs, 2016 - Taylor & Francis
Introduction: Prostate cancer is the most common cancer in elderly males. Regardless of the
initial hormonal treatment in metastatic disease, a significant proportion of patients develop …