Differential Expression of OATP1B3 Mediates Unconjugated Testosterone Influx.

ABSTRACT: Castration-resistant prostate cancer (CRPC) has greater intratumoral testosterone concentrations than similar tumors from eugonadal men; simple diffusion does not account for this observation. This study was undertaken to ascertain the androgen uptake kinetics, functional, and clinical relevance of de novo expression of the steroid hormone transporter OATP1B3 (SLCO1B3). Experiments testing the cellular uptake of androgens suggest that testosterone is an excellent substrate of OATP1B3 (K_m = 23.2 μmol/L; V_max = 321.6 pmol/mg/minute), and cells expressing a doxycycline-inducible SLCO1B3 construct had greater uptake of a clinically relevant concentration of 3H-testosterone (50 nmol/L; 1.6-fold, P = 0.0027). When compared with S

SUBMITTER: Sissung TM 

PROVIDER: S-EPMC5540879 | biostudies-literature | 2017 Aug

REPOSITORIES: biostudies-literature