Investigating the anti-mineralocorticoid properties of synthetic progestins used in hormone therapy

Biochemical and Biophysical Research Communications

Volumn 433, Issue 3, 2013, Pages 305-310

  Africander, Donita ^a   Louw, Renate ^a   Hapgood, Janet P ^b  

^a STELLENBOSCH UNIVERSITY   (South Africa)

^b UNIVERSITY OF CAPE TOWN   (South Africa)

Author keywords

Affinity; Antagonist; Cardiovascular; Mineralocorticoid receptor; Progestin

Indexed keywords

ALPHA GLYCOLYTIC PROTEIN; GLUCOCORTICOID; MEDROXYPROGESTERONE ACETATE; MINERALOCORTICOID; MINERALOCORTICOID RECEPTOR; NORETHISTERONE ACETATE; OROSOMUCOID; OROSOMUCOID1; PLASMINOGEN ACTIVATOR INHIBITOR 1; PROTEIN; SPIRONOLACTONE; UNCLASSIFIED DRUG;

ANIMAL CELL; ANIMAL TISSUE; ARTICLE; DRUG POTENCY; GENE; HORMONAL THERAPY; NONHUMAN; PRIORITY JOURNAL; RAT; RISK FACTOR; TRANSACTIVATION;

ANIMALS; ANTINEOPLASTIC AGENTS, HORMONAL; CELL LINE; CERCOPITHECUS AETHIOPS; CONTRACEPTIVES, ORAL, SYNTHETIC; COS CELLS; GENE EXPRESSION REGULATION; GENES, REPORTER; HUMANS; LUCIFERASES; MEDROXYPROGESTERONE ACETATE; MYOCYTES, CARDIAC; NORETHINDRONE; OROSOMUCOID; PLASMIDS; PLASMINOGEN ACTIVATOR INHIBITOR 1; RATS; RECEPTORS, MINERALOCORTICOID; RESPONSE ELEMENTS; SIGNAL TRANSDUCTION; TRANSCRIPTION, GENETIC; TRANSFECTION;

EID: 84876305464     PISSN: 0006291X     EISSN: 10902104     Source Type: Journal    
DOI: 10.1016/j.bbrc.2013.02.086     Document Type: Article

References (31)

1. Africander D., Verhoog N., Hapgood J.P. Molecular mechanisms of steroid receptor-mediated actions by synthetic progestins used in HRT and contraception. Steroids 2011, 76:636-652.
2. Hapgood J.P. Immunosuppressive biological mechanisms support reassessment of use of the injectable contraceptive medroxyprogesterone acetate. Endocrinology 2013, 154:985-988.
3. Hapgood J.P., Dominique K., Louw A., et al. Not all progestins are the same: implications for usage. Trends Pharmacol. Sci. 2004, 25:554-557.
4. F.Z. Stanczyk, J.P. Hapgood, S. Winer, D.R. Mishell Jr., Progestogens used in postmenopausal hormone therapy: differences in their pharmacological properties, intracellular actions, and clinical effects. Endocr Rev. 2012. [Epub ahead of print].
5. Warren M.P. A comparative review of the risks and benefits of hormone replacement therapy regimens. Am. J. Obstet. Gynecol. 2004, 190:1141-1167.
6. Beral V., Banks E., Bull D., et al. Breast cancer and hormone-replacement therapy in the Million Women Study. Lancet 2003, 362:419-427.
7. Heffron R., Donnell D., Celum C., et al. Use of hormonal contraceptives and risk of HIV-1 transmission: a prospective cohort study. Lancet Infect. Dis. 2012, 12:19-26.
8. Rossouw J.E., Anderson G.L., Prentice R.L., et al. Risks and benefits of estrogen plus progestin in healthy postmenopausal women: principal results from the Women's Health Initiative randomized controlled trial. JAMA 2002, 288:321-333.
9. Sorensen M.B., Collins P., Ong P.J., et al. Long-term use of contraceptive depot medroxyprogesterone acetate in young women impairs arterial endothelial function assessed by cardiovascular magnetic resonance. Circulation 2002, 106:1646-1651.
10. Lu N.Z., Wardell S.E., Burnstein K.L., et al. International union of pharmacology. LXV. The pharmacology and classification of the nuclear receptor superfamily: glucocorticoid, mineralocorticoid, progesterone, and androgen receptors. Pharmacol. Rev. 2006, 58:782-797.
11. Funder J.W. Aldosterone and mineralocorticoid receptors in the cardiovascular system. Prog. Cardiovasc. Dis. 2010, 52:393-400.
12. He B.J., Anderson M.E. Aldosterone and cardiovascular disease: the heart of the matter. Trends Endocrinol. Metab. 2013, 24:21-30.
13. Fejes-Tóth G., Náray-Fejes-Tóth A. Early aldosterone-regulated genes in cardiomyocytes: clues to cardiac remodeling?. Endocrinology 2007, 148:1502-1510.
14. Sui X., Bramlett K.S., Jorge M.C., et al. Specific androgen receptor activation by an artificial coactivator. J. Biol. Chem. 1999, 274:9449-9454.
15. Arriza J.L., Weinberger C., Cerelli G., et al. Cloning of human mineralocorticoid receptor complementary DNA: structural and functional kinship with the glucocorticoid receptor. Science 1987, 237:268-275.
16. Avenant C., Ronacher K., Stubsrud E., et al. Role of ligand-dependent GR phosphorylation and half-life in determination of ligand-specific transcriptional activity. Mol. Cell. Endocrinol. 2010, 327:72-88.
17. Bamberger C.M., Bamberger A.M., de Castro M., et al. Glucocorticoid receptor beta, a potential endogenous inhibitor of glucocorticoid action in humans. J. Clin. Invest. 1995, 95:2435-2441.
18. Cheng Y., Prusoff W.H. Relationship between the inhibition constant (K1) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction. Biochem. Pharmacol. 1973, 22:3099-3108.
19. Africander D., Louw R., Verhoog N., et al. Differential regulation of endogenous pro-inflammatory cytokine genes by medroxyprogesterone acetate and norethisterone acetate in cell lines of the female genital tract. Contraception 2011, 84:423-435.
20. Hagiwari H., Kaizu K., Uriu K., et al. Expression of type-1 plasminogen activator inhibitor in the kidney of diabetic rat models. Thromb. Res. 2003, 111:301-309.
21. Rupprecht R., Reul J.M., van Steensel B., et al. Pharmacological and functional characterization of human mineralocorticoid and glucocorticoid receptor ligands. Eur. J. Pharmacol. 1993, 247:145-154.
22. Philibert D., Bouchoux F., Degryse M., et al. The pharmacological profile of a novel norpregnance progestin (trimegestone). Gynecol. Endocrinol. 1999, 13:316-326.
23. Winneker R.C., Bitran D., Zhang Z. The preclinical biology of a new potent and selective progestin: trimegestone. Steroids 2003, 68:915-920.
24. Geller D.S., Farhi A., Pinkerton N., et al. Activating mineralocorticoid receptor mutation in hypertension exacerbated by pregnancy. Science 2000, 289:119-123.
25. Sasagawa S., Shimizu Y., Kami H., et al. Dienogest is a selective progesterone receptor agonist in transactivation analysis with potent oral endometrial activity due to its efficient pharmacokinetic profile. Steroids 2008, 73:222-231.
26. Rowlands S. Newer progestogens. J. Fam. Plann. Reprod. Health Care. 2003, 29:13-16.
27. Pearce D., Yamamoto K.R. Mineralocorticoid and glucocorticoid receptor activities distinguished by nonreceptor factors at a composite response element. Science 1993, 259:1161-1165.
28. Brown N.J., Vaughan D.E., Fogo A.B. Aldosterone and PAI-1: implications for renal injury. J. Nephrol. 2002, 15:230-235.
29. Engstrom G., Stavenow L., Hedblad B., et al. Inflammation-sensitive plasma proteins, diabetes, and mortality and incidence of myocardial infarction and stroke: a population-based study. Diabetes 2003, 52:442-447.
30. Koubovec D., Ronacher K., Stubsrud E., et al. Synthetic progestins used in HRT have different glucocorticoid agonist properties. Mol. Cell. Endocrinol. 2005, 242:23-32.
31. Lidegaard O., Lokkegaard E., Svendsen A.L., et al. Hormonal contraception and risk of venous thromboembolism: national follow-up study. BMJ 2009, 339:b2890.