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The estrogen receptor-alpha agonist 16alpha-LE2 inhibits cardiac hypertrophy and improves hemodynamic function in estrogen-deficient spontaneously hypertensive rats.
Pelzer T, Jazbutyte V, Hu K, Segerer S, Nahrendorf M, Nordbeck P, Bonz AW, Muck J, Fritzemeier KH, Hegele-Hartung C, Ertl G, Neyses L. Pelzer T, et al. Cardiovasc Res. 2005 Sep 1;67(4):604-12. doi: 10.1016/j.cardiores.2005.04.035. Cardiovasc Res. 2005. PMID: 15950203
The observed effects of E2 and 16alpha-LE2 were abrogated by the ER antagonist ZM-182780. Improved left ventricular function upon 16alpha-LE2 treatment was also observed in cardiac MRI studies. In contrast to estradiol and 16alpha-LE2, ta …
The observed effects of E2 and 16alpha-LE2 were abrogated by the ER antagonist ZM-182780. Improved left ventricular function u …
Effects of estrogen, an ERα agonist and raloxifene on pressure overload induced cardiac hypertrophy.
Westphal C, Schubert C, Prelle K, Penkalla A, Fliegner D, Petrov G, Regitz-Zagrosek V. Westphal C, et al. PLoS One. 2012;7(12):e50802. doi: 10.1371/journal.pone.0050802. Epub 2012 Dec 5. PLoS One. 2012. PMID: 23227210 Free PMC article.
E2, 16alpha-LE2 and raloxifene supported maintenance of cardiac function in comparison with placebo. ...E2 and 16alpha-LE2, but not raloxifene diminished the development of fibrosis and reduced the TGFbeta and CTGF gene expression. ...
E2, 16alpha-LE2 and raloxifene supported maintenance of cardiac function in comparison with placebo. ...E2 and 16alpha- …
Reporter cell lines to evaluate the selectivity of chemicals for human and zebrafish estrogen and peroxysome proliferator activated γ receptors.
Grimaldi M, Boulahtouf A, Delfosse V, Thouennon E, Bourguet W, Balaguer P. Grimaldi M, et al. Front Neurosci. 2015 Jun 9;9:212. doi: 10.3389/fnins.2015.00212. eCollection 2015. Front Neurosci. 2015. PMID: 26106289 Free PMC article. Review.
Some environmental estrogens (bisphenol A, mycoestrogens) which are hER panagonists displayed greater potency for zfERalpha as compared to zfERbetas. hERbeta selective agonists (8betaVE2, DPN, phytoestrogens) also displayed zfERalpha selectivity. Among hERalpha selective syntheti …
Some environmental estrogens (bisphenol A, mycoestrogens) which are hER panagonists displayed greater potency for zfERalpha as compared to z …
Estrogen receptor subtype-specific effects on markers of bone homeostasis.
Hertrampf T, Schleipen B, Velders M, Laudenbach U, Fritzemeier KH, Diel P. Hertrampf T, et al. Mol Cell Endocrinol. 2008 Sep 10;291(1-2):104-8. doi: 10.1016/j.mce.2008.03.003. Epub 2008 Mar 16. Mol Cell Endocrinol. 2008. PMID: 18433985
To further elucidate the processes involved in the physiology of bone-protection by estrogens, ovariectomized (OVX) rats were treated subcutaneously with 17beta-estradiol (E(2)), the ERalpha-specific agonist (16alpha-LE2) and the ERbeta-specific agonist (8beta-VE2). …
To further elucidate the processes involved in the physiology of bone-protection by estrogens, ovariectomized (OVX) rats were treated subcut …
Endogenous estrogen regulation of inflammatory arthritis and cytokine expression in male mice, predominantly via estrogen receptor alpha.
Yang YH, Ngo D, Jones M, Simpson E, Fritzemeier KH, Morand EF. Yang YH, et al. Arthritis Rheum. 2010 Apr;62(4):1017-25. doi: 10.1002/art.27330. Arthritis Rheum. 2010. PMID: 20131258 Free article.
RESULTS: Estrogen deficiency in ArKO mice was associated with significant increases in LPS-induced serum interleukin-6 (IL-6), tumor necrosis factor, monocyte chemotactic protein 1, and interferon-gamma levels, which were significantly abrogated by administration of 16alpha …
RESULTS: Estrogen deficiency in ArKO mice was associated with significant increases in LPS-induced serum interleukin-6 (IL-6), tumor necrosi …
Selectivity of natural, synthetic and environmental estrogens for zebrafish estrogen receptors.
Pinto C, Grimaldi M, Boulahtouf A, Pakdel F, Brion F, Aït-Aïssa S, Cavaillès V, Bourguet W, Gustafsson JA, Bondesson M, Balaguer P. Pinto C, et al. Toxicol Appl Pharmacol. 2014 Oct 1;280(1):60-9. doi: 10.1016/j.taap.2014.07.020. Epub 2014 Aug 8. Toxicol Appl Pharmacol. 2014. PMID: 25106122 Free PMC article.
Among hERalpha selective synthetic agonists, PPT did not activate zfERalpha while 16alpha-LE2 was the most zfERalpha selective compound. Altogether, these results confirm that all hER ligands control in a similar manner the transcriptional activity of zfERs although …
Among hERalpha selective synthetic agonists, PPT did not activate zfERalpha while 16alpha-LE2 was the most zfERalpha selective …
The estrogen receptor-α is required and sufficient to maintain physiological glucose uptake in the mouse heart.
Arias-Loza PA, Kreissl MC, Kneitz S, Kaiser FR, Israel I, Hu K, Frantz S, Bayer B, Fritzemeier KH, Korach KS, Pelzer T. Arias-Loza PA, et al. Hypertension. 2012 Oct;60(4):1070-7. doi: 10.1161/HYPERTENSIONAHA.111.190389. Epub 2012 Aug 14. Hypertension. 2012. PMID: 22892812 Free PMC article.
Cardiac glucose uptake quantified in vivo by 18F-fluorodeoxyglucose positron emission tomography was strongly impaired in ovariectomized compared with gonadal intact female C57BL/6JO mice. The selective ERalpha agonist 16alpha-LE2 and the nonselective ERalpha and ER …
Cardiac glucose uptake quantified in vivo by 18F-fluorodeoxyglucose positron emission tomography was strongly impaired in ovariectomized com …
Selective estrogen receptor-β activation stimulates skeletal muscle growth and regeneration.
Velders M, Schleipen B, Fritzemeier KH, Zierau O, Diel P. Velders M, et al. FASEB J. 2012 May;26(5):1909-20. doi: 10.1096/fj.11-194779. Epub 2012 Jan 25. FASEB J. 2012. PMID: 22278942
OVX rats were simultaneously treated with the ER-selective ligands genistein, ERalpha agonist 16alpha-LE2 (alpha), ERbeta agonist 8beta-VE2 (beta), or 17beta-estradiol (E(2)). ...
OVX rats were simultaneously treated with the ER-selective ligands genistein, ERalpha agonist 16alpha-LE2 (alpha), ERbeta agon …
Both estrogen receptor subtypes, ERα and ERβ, prevent aldosterone-induced oxidative stress in VSMC via increased NADPH bioavailability.
Muehlfelder M, Arias-Loza PA, Fritzemeier KH, Pelzer T. Muehlfelder M, et al. Biochem Biophys Res Commun. 2012 Jul 13;423(4):850-6. doi: 10.1016/j.bbrc.2012.06.053. Epub 2012 Jun 16. Biochem Biophys Res Commun. 2012. PMID: 22713467
In support of this concept, aldosterone increased ROS generation in vascular smooth muscle cells as determined by quantitative dihydroethidium fluorescence microscopy. Co-treatment with the selective ERalpha agonist 16alpha-LE2, the selective ERbeta agonist 8beta-VE …
In support of this concept, aldosterone increased ROS generation in vascular smooth muscle cells as determined by quantitative dihydroethidi …
Estrogens regulate neuroinflammatory genes via estrogen receptors α and β in the frontal cortex of middle-aged female rats.
Sárvári M, Hrabovszky E, Kalló I, Solymosi N, Tóth K, Likó I, Széles J, Mahó S, Molnár B, Liposits Z. Sárvári M, et al. J Neuroinflammation. 2011 Jul 20;8:82. doi: 10.1186/1742-2094-8-82. J Neuroinflammation. 2011. PMID: 21774811 Free PMC article.
RESULTS: Microarray analysis revealed the transcriptional regulation of 21 immunity/inflammation genes by 16alpha-LE2. The subsequent comparative real-time PCR study analyzed the isotype specific effects of ER agonists on neuroinflammatory genes of primarily glial o …
RESULTS: Microarray analysis revealed the transcriptional regulation of 21 immunity/inflammation genes by 16alpha-LE2. The sub …
16 results