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Molecular mechanisms of steroid receptor-mediated actions by synthetic progestins used in HRT and contraception
TLDR
The molecular mechanisms of intracellular actions of old (MPA, norethisterone, levonorgestrel, gestodene) vs. new (drospirenone, dienogest, trimegestone) generation progestins, via steroid receptors are reviewed. Expand
11β-Hydroxydihydrotestosterone and 11-ketodihydrotestosterone, novel C19 steroids with androgenic activity: A putative role in castration resistant prostate cancer?
TLDR
The data demonstrates that, while 11OHA4 has negligible androgensic activity, its metabolism to 11KT and 11KDHT yields androgenic compounds which may be implicated, together with A4 and DHEA(S), in driving CRPC in the absence of testicular T. Expand
Abrogation of Glucocorticoid Receptor Dimerization Correlates with Dissociated Glucocorticoid Behavior of Compound A*
TLDR
Comparison of the behavior of CpdA in the presence of wild type GR to that of Dex with a dimerization-deficient GR mutant (GRdim) strongly supports the conclusion that loss of Dimerization is responsible for the dissociated behavior ofCpdA. Expand
Potency of progestogens used in hormonal therapy: Toward understanding differential actions
TLDR
This review evaluates the usage, meaning and significance of the terms affinity, potency and efficacy in different models systems, with a view to improved understanding of their physiological and pharmacological significance. Expand
Not all progestins are the same: implications for usage.
TLDR
The molecular mechanisms of action of the relatively nonspecific and most widely used synthetic progestins, medroxyprogesterone acetate and norethisterone, are discussed and future directions involving a more mechanism-based approach for improved therapeutics, with greater specificity and fewer side-effects are discussed. Expand
The Injectable-Only Contraceptive Medroxyprogesterone Acetate, Unlike Norethisterone Acetate and Progesterone, Regulates Inflammatory Genes in Endocervical Cells via the Glucocorticoid Receptor
TLDR
These findings suggest that in the context of the genital mucosa, these GR-mediated glucocorticoid-like effects of MPA in cervical epithelial cells are likely to play a critical role in discriminating between the effects on inflammation caused by different progestins and P4 and hence susceptibility to genital infections. Expand
Differential regulation of endogenous pro-inflammatory cytokine genes by medroxyprogesterone acetate and norethisterone acetate in cell lines of the female genital tract.
TLDR
This study is the first to show ligand-, promoter- and cell-specific regulation of IL-6, IL-8 and RANTES gene expression by Prog, MPA and NET-A in these cell lines, and highlights the importance of choice of progestins for immune function in the cervicovaginal environment. Expand
Investigating the anti-mineralocorticoid properties of synthetic progestins used in hormone therapy.
TLDR
The results suggest that these progestins are unlikeley to exert significant effects via the MR at doses used in hormonal therapy, however, considering their relative free concentrations compared to endogenous hormones, the possibility that NET-A may exhibit significant MR antagonist activity, with some possible cardiovascular protective benefits, should not be excluded. Expand
Medroxyprogesterone Acetate Differentially Regulates Interleukin (IL)-12 and IL-10 in a Human Ectocervical Epithelial Cell Line in a Glucocorticoid Receptor (GR)-dependent Manner*
TLDR
The results suggest that both P4 and MPA may modulate inflammation in the ectocervix via this genomic mechanism, as both MPA and P4 favors a pro-inflammatory milieu in ectOCervical epithelial cells. Expand
A comparative characterization of estrogens used in hormone therapy via estrogen receptor (ER)-α and -β
TLDR
This study is the first to demonstrate that the bioidentical estrogens, commercially available estrogen standards and synthetic EE are full agonists for transrepression on both minimal and endogenous NFκB-containing promoters, suggesting that there is no clear advantage in choosing bHT above conventional HT. Expand
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