Inhibition of transforming growth factor (TGF)-β1–induced extracellular matrix with a novel inhibitor of the TGF-β type I receptor kinase activity: SB-431542

NJ Laping, E Grygielko, A Mathur, S Butter… - Molecular …, 2002 - ASPET
Transforming growth factor β1 (TGF-β1) is a potent fibrotic factor responsible for the
synthesis of extracellular matrix. TGF-β1 acts through the TGF-β type I and type II receptors to …

[HTML][HTML] Oral administration of GW788388, an inhibitor of TGF-β type I and II receptor kinases, decreases renal fibrosis

…, M Thorikay, M Deckers, M Van Dinther, ET Grygielko… - Kidney international, 2008 - Elsevier
Progressive kidney fibrosis precedes end-stage renal failure in up to a third of patients with
diabetes mellitus. Elevated intra-renal transforming growth factor-β (TGF-β) is thought to …

Novel Rho kinase inhibitors with anti-inflammatory and vasodilatory activities

…, D Jung, M Bamford, T Panchal, E Grygielko… - … of Pharmacology and …, 2007 - ASPET
Increased Rho kinase (ROCK) activity contributes to smooth muscle contraction and regulates
blood pressure homeostasis. We hypothesized that potent and selective ROCK inhibitors …

Inhibition of gene markers of fibrosis with a novel inhibitor of transforming growth factor-β type I receptor kinase in puromycin-induced nephritis

ET Grygielko, WM Martin, C Tweed, P Thornton… - … of Pharmacology and …, 2005 - ASPET
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 transforming growth factor-β1 (TGF-…

Human-induced pluripotent stem cell-derived cardiomyocytes exhibit temporal changes in phenotype

…, S Needle, ET Grygielko, E Hu… - American Journal …, 2013 - journals.physiology.org
Human-induced pluripotent stem cell-derived cardiomyocytes (hiPS-CMs) have been
recently derived and are used for basic research, cardiotoxicity assessment, and phenotypic …

A Structural and in Vitro Characterization of Asoprisnil: A Selective Progesterone Receptor Modulator

KP Madauss, ET Grygielko, SJ Deng… - Molecular …, 2007 - academic.oup.com
… Because the cellular data suggested that asoprisnil was a weak partial agonist, we
examined the ability of asoprisnil to oppose E 2 in the rat uterotrophic model. In this model, P 4 …

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 …

…, C Bertho-Ruault, A Patikis, ET Grygielko… - Journal of medicinal …, 2006 - ACS Publications
… The amido compounds 13a−e were synthesized by coupling the acid 9 with amines in
the presence of 1-hydroxybenzotriazole (HOBT) and 1-ethyl-3-(3-dimethylaminopropyl)…

Osmolality: a physiological long-term regulator of lumbar sympathetic nerve activity and arterial pressure

KE Scrogin, ET Grygielko… - American Journal of …, 1999 - journals.physiology.org
Acute infusion of hypertonic fluid increases mean arterial pressure (MAP) in part by elevating
nonrenal sympathetic activity. However, it is not known whether chronic, physiological …

Inhibition of ALK5 signaling induces physeal dysplasia in rats

…, R Boyce, D Zimmerman, E Grygielko… - Toxicologic …, 2007 - journals.sagepub.com
TGF-|β|, and its type 1 (ALK5) receptor, are critical to the pathogenesis of fibrosis. In toxicologic
studies of 4 or more days in 10-week-old Sprague–Dawley rats, using an ALK5 inhibitor (…

Estrogen-induced stromal cell-derived factor-1 (SDF-1/Cxcl12) expression is repressed by progesterone and by Selective Estrogen Receptor Modulators via estrogen …

L Glace, ET Grygielko, R Boyle, Q Wang, NJ Laping… - Steroids, 2009 - Elsevier
Endometriosis, defined as the presence of endometrial glands and stroma at extra-uterine
sites, is a gynecological condition that affects women of reproductive age. Consistent with its …