Molecular mechanisms of steroid receptor-mediated actions by synthetic progestins used in HRT and contraception

@article{Africander2011MolecularMO,
  title={Molecular mechanisms of steroid receptor-mediated actions by synthetic progestins used in HRT and contraception},
  author={Donita Africander and Nicolette J.D. Verhoog and Janet P. Hapgood},
  journal={Steroids},
  year={2011},
  volume={76},
  pages={636-652}
}
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References

SHOWING 1-10 OF 228 REFERENCES

Disruption of androgen receptor signaling by synthetic progestins may increase risk of developing breast cancer

It is proposed that the observed excess of breast malignancies associated with combined HRT may be explained, in part, by synthetic progestins such as MPA acting as endocrine disruptors to negate the protective effects of androgen signaling in the breast.

Pharmacology of different progestogens: the special case of drospirenone

  • R. Sitruk-Ware
  • Biology, Medicine
    Climacteric : the journal of the International Menopause Society
  • 2005
Drospirenone, which has pharmacodynamic properties very similar to those of progesterone, has been developed as a combined oral contraceptive and may counteract the negative effect of androgens on hair growth, lipid changes, insulin and, possibly, body composition in postmenopausal women.

Pharmacology of estrogens and progestogens: influence of different routes of administration

  • H. Kuhl
  • Medicine, Biology
    Climacteric : the journal of the International Menopause Society
  • 2005
This review comprises the pharmacokinetics and pharmacodynamics of natural and synthetic estrogens and progestogens used in contraception and therapy, with special consideration of hormone…

Progestins and cardiovascular risk markers

The progestational and androgenic properties of medroxyprogesterone acetate: gene regulatory overlap with dihydrotestosterone in breast cancer cells

Clinically, the complex pharmacology of MPA not only influences its side-effect profile; but it is also possible that the increased breast cancer risk and/or the therapeutic efficacy of M PA in cancer treatment is in part mediated by androgen receptor.

Mechanism of action of contraceptive synthetic progestins.

Androgen receptor agonist activity of the synthetic progestin, medroxyprogesterone acetate, in human breast cancer cells

Conception and pharmacodynamic profile of drospirenone

Drospirenone: pharmacology and pharmacokinetics of a unique progestogen.

Steroid hormone receptors: an update.

By all these different mechanisms SHRs modulate numerous and specific responses in a large variety of cells, whereby their particular effect depends on the physiological, cellular and genetic context.
...