Comparing the androgenic and estrogenic properties of progestins used in contraception and hormone therapy.

ABSTRACT: Progestins used in endocrine therapies bind to multiple steroid receptors and are associated with several side-effects. It is thus important to understand the relationship between steroid receptor cross-reactivity and the side-effect profile of progestins. In cell lines that express negligible levels of steroid receptors, we report for the first time the binding affinities, potencies and efficacies of selected progestins from different generations determined in parallel. We show that the progestins bind to the androgen receptor (AR) with similar affinities to each other and progesterone, while none bind estrogen receptor (ER)-β, and only norethisterone acetate, levonorgestrel and gestodene bind ERα. Comparative dose-response analysis revealed that progestins from the first three generation

SUBMITTER: Louw-du Toit R 

PROVIDER: S-EPMC5740213 | biostudies-literature | 2017 Sep

REPOSITORIES: biostudies-literature