Androgen receptor: structure, role in prostate cancer and drug discovery
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 …
phenotype. Several diseases, such as androgen insensitivity syndrome (AIS) and prostate …
Therapeutic strategies to target the androgen receptor
The androgen receptor (AR) plays a key role in the maintenance of muscle and bone and
the support of male sexual-related functions, as well as in the progression of prostate …
the support of male sexual-related functions, as well as in the progression of prostate …
Oleic acid is an endogenous ligand of TLX/NR2E1 that triggers hippocampal neurogenesis
Neural stem cells, the source of newborn neurons in the adult hippocampus, are intimately
involved in learning and memory, mood, and stress response. Despite considerable …
involved in learning and memory, mood, and stress response. Despite considerable …
Best practices of computer-aided drug discovery: lessons learned from the development of a preclinical candidate for prostate cancer with a new mechanism of action
Small-molecule drug design is a complex and iterative decision-making process relying on
pre-existing knowledge and driven by experimental data. Low-molecular-weight chemicals …
pre-existing knowledge and driven by experimental data. Low-molecular-weight chemicals …
Targeting the binding function 3 (BF3) site of the human androgen receptor through virtual screening.
NA Lack, P Axerio-Cilies, P Tavassoli… - Journal of medicinal …, 2011 - ACS Publications
The androgen receptor (AR) is the best studied drug target for the treatment of prostate
cancer. While there are a number of drugs that target the AR, they all work through the same …
cancer. While there are a number of drugs that target the AR, they all work through the same …
Discovery of small-molecule inhibitors selectively targeting the DNA-binding domain of the human androgen receptor
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 …
and progression of prostate cancer (PCa). As resistance to clinically used anti-AR drugs …
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 …
including the cancers of prostate, breast, ovary, pancreas, etc and anabolic deficiencies …
Discovery of new catalytic topoisomerase II inhibitors for anticancer therapeutics
VM Matias-Barrios, M Radaeva, Y Song… - Frontiers in …, 2021 - frontiersin.org
Poison inhibitors of DNA topoisomerase II (TOP2) are clinically used drugs that cause
cancer cell death by inducing DNA damage, which mechanism of action is also associated …
cancer cell death by inducing DNA damage, which mechanism of action is also associated …
Isomerization of bioactive acylhydrazones triggered by light or thiols
The acylhydrazone unit is well represented in screening databases used to find ligands for
biological targets, and numerous bioactive acylhydrazones have been reported. However …
biological targets, and numerous bioactive acylhydrazones have been reported. However …
Computer-aided ligand discovery for estrogen receptor alpha
D Bafna, F Ban, PS Rennie, K Singh… - International Journal of …, 2020 - mdpi.com
Breast cancer (BCa) is one of the most predominantly diagnosed cancers in women.
Notably, 70% of BCa diagnoses are Estrogen Receptor α positive (ERα+) making it a critical …
Notably, 70% of BCa diagnoses are Estrogen Receptor α positive (ERα+) making it a critical …