Search Results - "Grygielko, Eugene T"
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Human-induced pluripotent stem cell-derived cardiomyocytes exhibit temporal changes in phenotype
Published in American journal of physiology. Heart and circulatory physiology (15-09-2013)“…Human-induced pluripotent stem cell-derived cardiomyocytes (hiPS-CMs) have been recently derived and are used for basic research, cardiotoxicity assessment,…”
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2
A Structural and in Vitro Characterization of Asoprisnil: A Selective Progesterone Receptor Modulator
Published in Molecular endocrinology (Baltimore, Md.) (01-05-2007)“…Selective progesterone receptor modulators (SPRMs) have been suggested as therapeutic agents for treatment of gynecological disorders. One such SPRM,…”
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3
Inhibition of gene markers of fibrosis with a novel inhibitor of transforming growth factor-beta type I receptor kinase in puromycin-induced nephritis
Published in The Journal of pharmacology and experimental therapeutics (01-06-2005)“…SB-525334 (6-[2-tert-butyl-5-(6-methyl-pyridin-2-yl)-1H-imidazol-4-yl]-quinoxaline) has been characterized as a potent and selective inhibitor of the…”
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4
Osmolality: a physiological long-term regulator of lumbar sympathetic nerve activity and arterial pressure
Published in The American journal of physiology (01-06-1999)“…Acute infusion of hypertonic fluid increases mean arterial pressure (MAP) in part by elevating nonrenal sympathetic activity. However, it is not known whether…”
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5
Discovery of 4-{4-[3-(Pyridin-2-yl)-1H-pyrazol-4-yl]pyridin-2-yl}-N-(tetrahydro-2H- pyran-4-yl)benzamide (GW788388): A Potent, Selective, and Orally Active Transforming Growth Factor-β Type I Receptor Inhibitor
Published in Journal of medicinal chemistry (06-04-2006)“…Inhibitors of transforming growth factor β (TGF-β) type I receptor (ALK5) offer a novel approach for the treatment of fibrotic diseases such as renal, hepatic,…”
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6
The angiotensin type 1 receptor antagonist, eprosartan, attenuates the progression of renal disease in spontaneously hypertensive stroke-prone rats with accelerated hypertension
Published in The Journal of pharmacology and experimental therapeutics (01-04-2002)“…The effects of the angiotensin type 1 (AT(1)) receptor antagonist, eprosartan, were studied in a model of severe, chronic hypertension. Treatment of male…”
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7
Estrogen-induced stromal cell-derived factor-1 (SDF-1/ Cxcl12) expression is repressed by progesterone and by Selective Estrogen Receptor Modulators via estrogen receptor α in rat uterine cells and tissues
Published in Steroids (01-11-2009)“…Endometriosis, defined as the presence of endometrial glands and stroma at extra-uterine sites, is a gynecological condition that affects women of reproductive…”
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8
Effects of angiotensins II and IV on blood pressure, renal function, and PAI-1 expression in the heart and kidney of the rat
Published in Pharmacology (01-09-2002)“…The role of angiotensin II (AII) and angiotensin IV (AIV) as inducers of PAI-1 expression during hypertension was studied in vivo. A 2-week infusion of AII…”
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9
Rational design of orally-active, pyrrolidine-based progesterone receptor partial agonists
Published in Bioorganic & medicinal chemistry letters (15-08-2009)“…Using the X-ray crystal structure of an amide-based progesterone receptor (PR) partial agonist bound to the PR ligand binding domain, a novel PR partial…”
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10
2-Amino-9-aryl-3-cyano-4-methyl-7-oxo-6,7,8,9-tetrahydropyrido[2′,3′:4,5]thieno[2,3- b]pyridine derivatives as selective progesterone receptor agonists
Published in Bioorganic & medicinal chemistry letters (01-09-2009)“…A novel series of 2-amino-9-aryl-3-cyano-4-methyl-7-oxo-6,7,8,9-tetrahydropyrido[2′,3′:4,5]thieno[2,3- b]pyridine derivatives was identified as selective PR…”
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11
Synthesis and SAR of amino acid-derived heterocyclic progesterone receptor full and partial agonists
Published in Bioorganic & medicinal chemistry letters (15-05-2009)“…Two series of amino acid-derived heterocyclic progesterone receptor (PR) ligands are reported. Tetrazole-containing ligands behaved as potent PR partial…”
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12
Improving the developability profile of pyrrolidine progesterone receptor partial agonists
Published in Bioorganic & medicinal chemistry letters (01-01-2010)“…The previously reported pyrrolidine class of progesterone receptor partial agonists demonstrated excellent potency but suffered from serious liabilities…”
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13
Discovery of orally active, pyrrolidinone-based progesterone receptor partial agonists
Published in Bioorganic & medicinal chemistry letters (15-08-2009)“…We have designed and synthesized a novel series of pyrrolidinones as progesterone receptor partial agonists. Compounds from this series had improved AR…”
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14
Ganglionic tyrosine hydroxylase and norepinephrine transporter are decreased by increased sodium chloride in vivo and in vitro
Published in Autonomic neuroscience (30-09-2003)“…The present study tested the hypothesis that, in normal male rats, chronic changes in salt intake alter the levels of tyrosine hydroxylase and the…”
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15
Role of caspases in human renal proximal tubular epithelial cell apoptosis
Published in European journal of pharmacology (21-12-2001)“…In the present study, we have used an in vitro model of apoptosis using primary human renal proximal tubular epithelial (RPTE) cells to investigate the…”
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16
Compensatory role for Sgk2 mediated sodium reabsorption during salt deprivation in Sgk1 knockout mice
Published in The FASEB journal (01-04-2007)“…The purpose of this study was to investigate the role of Sgk2 in the regulation of salt and water homeostasis. Kidney function and expression of Sgk1, Sgk2,…”
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