Testosterone challenge and androgen receptor activity in relation to UGT2B17 genotypes
Version of Record online: 7 JAN 2013
© 2012 The Authors. European Journal of Clinical Investigation © 2012 Stichting European Society for Clinical Investigation Journal Foundation
European Journal of Clinical Investigation
Volume 43, Issue 3, pages 248–255, March 2013
How to Cite
Eur J Clin Invest 2013; 43 (3): 248–255
- Issue online: 14 FEB 2013
- Version of Record online: 7 JAN 2013
- Accepted manuscript online: 2 JAN 2013 12:30AM EST
- Manuscript Accepted: 27 NOV 2012
- Manuscript Received: 2 JUL 2012
- World Anti Doping Agency (WADA)
- Swedish Center for Sports Research
- Androgen receptor activity;
We investigated the androgen receptor (AR) bioluminescense response in serum and urine before and after testosterone challenge in different genotypes of the UGT2B17 enzyme, which catalyses testosterone glucuronidation.
Material and methods
The androgen receptor activity was determined using a yeast-based bioluminescence assay. The androgens were analysed using LC-MS/MS, and the individuals were genotyped for UGT2B17 deletion polymorphism using real-time polymerase chain reaction.
The serum concentrations of testosterone and dihydrotestosterone (DHT) were markedly elevated on days 2 and 4 and were still above baseline on day 15 after a dose of 500 mg testosterone enanthate. The androgenic activity in serum increased in parallel and correlated with the hormone concentrations and remained above baseline on day 15. The urinary androgenic activity increased 4–5-fold and was closely related to the unconjugated testosterone and independent of the UGT2B17 genotype.
The AR assay may serve as a complement to the urinary testosterone/epitestosterone (T/E) doping test, because this is profoundly influenced by the UGT2B17 deletion polymorphism. It may also be useful for detection of other illicit androgens in sports, or in the society, or for monitoring and diagnostics of androgen-related disorders.