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Hormones, Hormone Substitutes, and Hormone Antagonists (2)
Articles on Hormones, Hormone Substitutes, and Hormone Antagonists
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Prenylated isoflavonoids from plants as selective estrogen receptor modulators (phytoSERMs).
Food Funct 3(8):810-27 (2012) PMID 22684228
Isoflavonoids are a class of secondary metabolites, which comprise amongst others the subclasses of isoflavones, isoflavans, pterocarpans and coumestans. Isoflavonoids are abundant in Leguminosae, and many of them can bind to the human estrogen receptor (hER) with affinities similar... -
Novel pharmacological approaches to the treatment of type 2 diabetes.
Pharmacol Rev 64(2):188-237 (2012) PMID 22407617
The huge increase in type 2 diabetes is a burden worldwide. Many marketed compounds do not address relevant aspects of the disease; they may already compensate for defects in insulin secretion and insulin action, but loss of secreting cells (β-cell destruction), hyperglucagonemia, g... -
Cyanide is an adequate agonist of the plant hormone ethylene for studying signalling of sensor kinase ETR1 at the molecular level.
Biochem J 444(2):261-7 (2012) PMID 22390794
We show that cyanide, a π-acceptor compound and structural analogue of ethylene, is a suitable substitute for the plant hormone for in vitro studies with purified proteins. Recombinant ethylene receptor protein ETR1 showed high level and selective binding of radiolabelled [14C]cyanide in the presen... -
8-alkylthio-6-thio-substituted theophylline analogues as selective noncompetitive progesterone receptor antagonists.
Steroids 77(6):596-601 (2012) PMID 22421057
The progesterone receptor (PR) plays a key role in reproduction and is important in cancers of the reproductive tract. Current PR antagonists usually compete for progestin binding in the PR ligand-binding pocket and often exhibit cross-binding with other members of the steroid recept... -
Nutritional hepatic iron overload is not prevented by parenteral hepcidin substitution therapy in mice.
Br J Nutr 108(10):1723-5 (2012) PMID 22321247
We therefore tested whether multiple doses of intraperitoneally administered synthetic renatured hepcidin can prevent hepatic Fe loading in mice concurrently fed an Fe-rich diet, and whether the same treatment affects hepatic Fe stores in mice fed a normal diet. Cohorts of male mice were fed either... -
Kisspeptin inhibits high-voltage activated ca2+ channels in GnRH neurons via multiple ca2+ influx and release pathways.
Neuroendocrinology 96(1):68-80 (2012) PMID 22343183
We used whole-cell patch-clamp recording to examine the effects of kisspeptin-10 (KP-10) on VGCC activity evoked by step depolarizations in GnRH neurons in brain slices from pubertal male GnRH-green fluorescent protein transgenic mice. Prolonged (>30 s) KP-10 application inhibited Ca(2+) currents. T... -
The neuropharmacology of prolactin secretion elicited by 3,4-methylenedioxymethamphetamine ("ecstasy"): a concurrent microdialysis and plasm...
Horm Behav 61(2):181-90 (2012) PMID 22197270
We evaluated the role of the serotonin transporter and the 5-HT(2A) receptor in S,R(+/-)-MDMA- and R(-)-MDMA-elicited prolactin secretion in rhesus monkeys through concurrent microdialysis and plasma analysis determinations and drug interaction experiments. Concurrent neurochemical and hormone deter... -
Factors affecting the aldosterone/renin ratio.
Horm Metab Res 44(3):170-6 (2012) PMID 22147655
We recently reported selective serotonin reuptake inhibitors lower the ratio. Because potassium regulates aldosterone, uncorrected hypokalemia can lead to false negatives. Beta-blockers, alpha-methyldopa, clonidine, and nonsteroidal anti-inflammatory drugs suppress renin, raising the ARR with potent... -
Synthesis and antihormonal properties of novel 11β-benzoxazole-substituted steroids.
Bioorg Med Chem Lett 22(4):1705-8 (2012) PMID 22260770
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Silicon analogues of the nonpeptidic GnRH antagonist AG-045572: syntheses, crystal structure analyses, and pharmacological characterization.
ChemMedChem 6(11):2070-80 (2011) PMID 21953839
AG-045572 (CMPD1, 1 a) is a nonpeptidic gonadotropin-releasing hormone (GnRH) antagonist that has been investigated for the treatment of sex hormone-related diseases. In the context of systematic studies on sila-substituted drugs, the silicon analogue disila-AG-045572 (1 b) and its derivative 2 w...