Comparison of the three SARMs RAD-140, GLPG0492 and GSK-2881078 in two different in vitro bioassays, and in an in silico androgen receptor binding assay.
Androgen Antagonists
/ pharmacology
Androgens
/ pharmacology
Cell Line, Tumor
Computer Simulation
Drug Evaluation, Preclinical
/ methods
Humans
Hydantoins
/ pharmacology
Indoles
/ pharmacology
Molecular Docking Simulation
Nitriles
/ pharmacology
Oxadiazoles
/ pharmacology
Protein Binding
Receptors, Androgen
/ metabolism
Molecular modeling
PC3(AR)(2)cells
Selective androgen receptor modulators
Yeast androgen screen
Journal
The Journal of steroid biochemistry and molecular biology
ISSN: 1879-1220
Titre abrégé: J Steroid Biochem Mol Biol
Pays: England
ID NLM: 9015483
Informations de publication
Date de publication:
05 2019
05 2019
Historique:
received:
14
11
2018
revised:
28
01
2019
accepted:
26
02
2019
pubmed:
3
3
2019
medline:
22
11
2019
entrez:
3
3
2019
Statut:
ppublish
Résumé
Selective androgen receptor modulators comprise compounds that bind as ligands to the androgen receptor and possess tissue-selective activities. Ideally, they show agonistic properties in anabolic target tissues, while inducing antagonistic or only weak agonistic effects in reproductive organs. Due to their myoanabolic effects, selective androgen receptor modulators are included in the list of prohibited substances and methods of the World Anti-Doping Agency. In the current investigation, the androgenic potential of RAD-140, GSK-2881078 and GLPG0492 was comparably investigated in two different in vitro bioassays. In the yeast androgen screen, the androgenic effects were lower than in the reporter gene assay in prostate carcinoma cells (e.g. for GSK-2881078, the EC
Identifiants
pubmed: 30825507
pii: S0960-0760(18)30688-5
doi: 10.1016/j.jsbmb.2019.02.014
pii:
doi:
Substances chimiques
4-(4-(hydroxymethyl)-3-methyl-2,5-dioxo-4-phenylimidazolidin-1-yl)-2-(trifluoromethyl)benzonitrile
0
AR protein, human
0
Androgen Antagonists
0
Androgens
0
Hydantoins
0
Indoles
0
Nitriles
0
Oxadiazoles
0
Receptors, Androgen
0
GSK2881078
47M5ZXU844
RAD140
4O87Q44KNC
Types de publication
Comparative Study
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
81-86Informations de copyright
Copyright © 2019 Elsevier Ltd. All rights reserved.