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 …
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 …
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 …
(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 …
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 (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?
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 …
(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 …
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
Motivation Successful development and application of precision oncology approaches
require robust elucidation of the genomic landscape of a patient's cancer and, ideally, the …
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 …
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 …
initial hormonal treatment in metastatic disease, a significant proportion of patients develop …