Discovery of small-molecule inhibitors selectively targeting the DNA-binding domain of the human androgen receptor

H Li, F Ban, K Dalal, E Leblanc, K Frewin… - Journal of medicinal …, 2014 - ACS Publications
The human androgen receptor (AR) is considered as a master regulator in the development
and progression of prostate cancer (PCa). As resistance to clinically used anti-AR drugs …

Selective modulation of genomic and nongenomic androgen responses by androgen receptor ligands

LB Lutz, M Jamnongjit, WH Yang… - Molecular …, 2003 - academic.oup.com
Steroids can induce both transcription-dependent (genomic) and independent
(nongenomic) signaling. Here, several classical androgen receptor ligands were tested for …

[HTML][HTML] Selective androgen receptor modulators activate the canonical prostate cancer androgen receptor program and repress cancer growth

MD Nyquist, LS Ang, A Corella… - The Journal of …, 2021 - Am Soc Clin Investig
Prostate cancer (PC) is driven by androgen receptor (AR) activity, a master regulator of
prostate development and homeostasis. Frontline therapies for metastatic PC deprive the …

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 …

Basics of androgen synthesis and action

RN Elzenaty, T Du Toit, CE Flück - Best Practice & Research Clinical …, 2022 - Elsevier
Androgens are essential sex steroid hormones for both sexes. Testosterone (T) is the
predominant androgen in males, while in adult females, T concentrations are about 15-fold …

[引用][C] Clinical review 34: androgen treatment of hypogonadal men

S Bhasin - The Journal of Clinical Endocrinology & Metabolism, 1992 - academic.oup.com
Several remarkable advances in androgen phar-macology during the last decade, including
better understanding of the pharmacokinetics of testosterone esters and the development of …

New generation of selective androgen receptor degraders: our initial design, synthesis, and biological evaluation of new compounds with enzalutamide-resistant …

DJ Hwang, Y He, S Ponnusamy… - Journal of Medicinal …, 2018 - ACS Publications
In our effort to find small-molecule treatments of advanced prostate cancers (PCs), a novel
series of indolyl and indolinyl propanamides (series II and III) were discovered as selective …

Targeting the androgen receptor in prostate and breast cancer: several new agents in development

T Proverbs-Singh, JL Feldman… - Endocrine-related …, 2015 - erc.bioscientifica.com
Prostate cancer (PCa) and breast cancer (BCa) share similarities as hormone-sensitive
cancers with a wide heterogeneity of both phenotype and biology. The androgen receptor …

Androgen receptor structural and functional elements: role and regulation in prostate cancer

SM Dehm, DJ Tindall - Molecular endocrinology, 2007 - academic.oup.com
The androgen receptor (AR) is a nuclear receptor transcription factor that mediates the
cellular actions of androgens, the male sex steroids. Androgen-dependent tissues, such as …

Androgen receptor phosphorylation: biological context and functional consequences

Y Koryakina, HQ Ta, D Gioeli - Endocrine-related cancer, 2014 - erc.bioscientifica.com
The androgen receptor (AR) is a ligand-regulated transcription factor that belongs to the
family of nuclear receptors. In addition to regulation by steroid, the AR is also regulated by …