| Previous studies have reported that HIV-1 is capable of both acute and persistent infection in the testes. The naturally restrictive environment in the testes, due in part to the expression of drug transporters at the blood-testes-barrier (BTB), could limit antiretroviral (ARV) penetration into this tissue and contribute to the formation of a viral sanctuary. Therefore, we conducted a comprehensive characterization of gene and protein expression and localization of major drug transporters and metabolic enzymes relevant to ARV therapy in testicular tissue isolated from both uninfected and HIV-1 infected, treated individuals. We also quantified drug concentration levels in testicular tissue versus plasma to gain additional insight on ARV drug penetration into the testes. Overall, our findings indicate that the testes express many key drug transporters and metabolic enzymes relevant to ARV therapy, which could limit the penetration of certain ARV compounds, and contribute to persistent HIV-1 infection and formation of a viral sanctuary site. |