Androgen receptor: structure, role in prostate cancer and drug discovery

MH Tan, J Li, HE Xu, K Melcher, E Yong - Acta Pharmacologica Sinica, 2015 - nature.com
Androgens and androgen receptors (AR) play a pivotal role in expression of the male
phenotype. Several diseases, such as androgen insensitivity syndrome (AIS) and prostate …

In silico Strategies to Support Fragment-to-Lead Optimization in Drug Discovery

LR de Souza Neto, JT Moreira-Filho, BJ Neves… - Frontiers in …, 2020 - frontiersin.org
Fragment-based drug (or lead) discovery (FBDD or FBLD) has developed in the last two
decades to become a successful key technology in the pharmaceutical industry for early …

Structural features of tight-junction proteins

U Heinemann, A Schuetz - International journal of molecular sciences, 2019 - mdpi.com
Tight junctions are complex supramolecular entities composed of integral membrane
proteins, membrane-associated and soluble cytoplasmic proteins engaging in an intricate …

Boron in drug discovery: carboranes as unique pharmacophores in biologically active compounds

F Issa, M Kassiou, LM Rendina - Chemical reviews, 2011 - ACS Publications
Boron, in the form of boric acid, has played a role in medicine as a mild antiseptic and an
eye wash since its preparation from borax in the 18th century. However, the use of boron in …

The development of androgen-independent prostate cancer

BJ Feldman, D Feldman - Nature Reviews Cancer, 2001 - nature.com
The normal prostate and early-stage prostate cancers depend on androgens for growth and
survival, and androgen ablation therapy causes them to regress. Cancers that are not cured …

Molecular determinants of resistance to antiandrogen therapy

CD Chen, DS Welsbie, C Tran, SH Baek, R Chen… - Nature medicine, 2004 - nature.com
Using microarray-based profiling of isogenic prostate cancer xenograft models, we found
that a modest increase in androgen receptor mRNA was the only change consistently …

The androgen receptor gene mutations database: 2012 update

B Gottlieb, LK Beitel, A Nadarajah, M Paliouras… - Human …, 2012 - Wiley Online Library
The current version of the androgen receptor gene (AR) mutations database is described. A
major change to the database is that the nomenclature and numbering scheme now …

Splicing of a Novel Androgen Receptor Exon Generates a Constitutively Active Androgen Receptor that Mediates Prostate Cancer Therapy Resistance

SM Dehm, LJ Schmidt, HV Heemers, RL Vessella… - Cancer research, 2008 - AACR
The standard systemic treatment for prostate cancer (PCa) is androgen ablation, which
causes tumor regression by inhibiting activity of the androgen receptor (AR). Invariably, PCa …

Molecular biology of the androgen receptor

EP Gelmann - Journal of clinical oncology, 2002 - ascopubs.org
Androgen receptor (AR) is a member of the steroid hormone receptor family of molecules.
AR primarily is responsible for mediating the physiologic effects of androgens by binding to …

Androgen insensitivity syndrome

IA Hughes, JD Davies, TI Bunch, V Pasterski… - The Lancet, 2012 - thelancet.com
Androgen insensitivity syndrome in its complete form is a disorder of hormone resistance
characterised by a female phenotype in an individual with an XY karyotype and testes …