A direct comparison of the transcriptional activities of progestins used in contraception and menopausal hormone therapy via the mineralocorticoid receptor.

ABSTRACT: A variety of structurally and functionally distinct progestins is used in contraception and menopausal hormone therapy (MHT). Some progestins elicit off-target effects by binding to steroid receptors other than the progesterone receptor, which may impact their therapeutic and side-effect profiles. We directly compared the binding affinities, efficacies and potencies of selected progestins via the mineralocorticoid receptor (MR). We did not detect a significant difference in the affinities of medroxyprogesterone acetate (MPA), norethisterone acetate (NET-A), levonorgestrel (LNG), gestodene (GES), etonogestrel (ETG), nestorone (NES) and nomegestrel acetate (NoMAC) for the MR, while these were significantly lower compared to drospirenone (DRSP). While GES and NoMAC display affinities indistin

SUBMITTER: Louw-du Toit R 

PROVIDER: S-EPMC7287572 | biostudies-literature | 2020 May

REPOSITORIES: biostudies-literature