Výsledky vyhledávání - "Eugene T. Grygielko"

Discovery of orally active, pyrrolidinone-based progesterone receptor partial agonists

Autor: Rakesh Nagilla, Sharada Manns, Eugene L. Stewart, Marlys Hammond, Tram H. Hoang, Scott K. Thompson, Walter Trizna, Chaya Duraiswami, Eugene T. Grygielko, Thuy B. Tran, James S. Frazee, Kevin P. Madauss, Johnson Latisha C, Shawn P. Williams, Lindsay E. Glace, David G. Washburn, Jeffrey D. Bray

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 19:4664-4668

We have designed and synthesized a novel series of pyrrolidinones as progesterone receptor partial agonists. Compounds from this series had improved AR selectivity, rat pharmacokinetic properties, and in vivo potency compared to the lead compound. In

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4e117925c53a26178fac52da1fa94885
https://doi.org/10.1016/j.bmcl.2009.06.081

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

Autor: Eugene T. Grygielko, Eugene L. Stewart, Jeffrey D. Bray, Nicholas J. Laping, Charlene Wu, Shawn P. Williams, Thomas B. Stanley, Kevin P. Madauss, Su-Jun Deng, Steve A. Short, Anthony Sulpizio, Scott K. Thompson

Publikováno v: Molecular Endocrinology. 21:1066-1081

Selective progesterone receptor modulators (SPRMs) have been suggested as therapeutic agents for treatment of gynecological disorders. One such SPRM, asoprisnil, was recently in clinical trials for treatment of uterine fibroids and endometriosis. We

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::07c51747593a2c6b0898680d9bb76c25
https://doi.org/10.1210/me.2006-0524

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Inhibition of ALK5 Signaling Induces Physeal Dysplasia in Rats

Autor: Roberta A. Thomas, Kendall S. Frazier, Stephane Huet, Nicholas J. Laping, Françoise Gellibert, Rogely W. Boyce, Anne-Charlotte DeGouville, James Nold, Rosanna C. Mirabile, Dawn Zimmerman, Marshall S. Scicchitano, Eugene T. Grygielko

Publikováno v: Toxicologic Pathology. 35:284-295

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 (GW788388), expansion of hypertrophic and proliferation zon

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::05a2b210048b9e11ba1dbf11cc237eb6
https://doi.org/10.1080/01926230701198469

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Novel Rho Kinase Inhibitors with Anti-inflammatory and Vasodilatory Activities

Publikováno v: Journal of Pharmacology and Experimental Therapeutics. 320:89-98

Increased Rho kinase (ROCK) activity contributes to smooth muscle contraction and regulates blood pressure homeostasis. We hypothesized that potent and selective ROCK inhibitors with novel structural motifs would help elucidate the functional role of

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5dce38430c139758cf6d25985f84a50d
https://doi.org/10.1124/jpet.106.110635

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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

Autor: James Michael Woolven, Eugene T. Grygielko, FranÃ§oise Gellibert, Neil Mathews, StÃ©phane Huet, Nicholas J. Laping, Angela Patikis, CÃ©cile Bertho-Ruault, Anne-Charlotte de Gouville, Van-Loc Nguyen

Publikováno v: Journal of Medicinal Chemistry. 49:2210-2221

Inhibitors of transforming growth factor beta (TGF-beta) type I receptor (ALK5) offer a novel approach for the treatment of fibrotic diseases such as renal, hepatic, and pulmonary fibrosis. The optimization of a novel phenylpyridine pyrazole series (

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::114d01271eafa1afb68f20a7a2c7cc1a
https://doi.org/10.1021/jm0509905

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Ganglionic tyrosine hydroxylase and norepinephrine transporter are decreased by increased sodium chloride in vivo and in vitro

Autor: Virginia L. Brooks, Timothy A. Huhtala, Beth A. Habecker, Billy Foote, Eugene T. Grygielko

Publikováno v: Autonomic Neuroscience. 107:85-98

The present study tested the hypothesis that, in normal male rats, chronic changes in salt intake alter the levels of tyrosine hydroxylase and the norepinephrine transporter in sympathetic ganglia. Increasing dietary salt (from 0.02% to 1%, 4% or 8%

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::187489ebe09ceb025c59f5c662b52ffa
https://doi.org/10.1016/s1566-0702(03)00133-4

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

Autor: John R. Toomey, Eugene T. Grygielko, John J. Lepore, Zuojun Lin, Saul Needle, Erding Hu, Gordon C. Teg Pipes, Irina M. Lozinskaya, Christine Y. Ivashchenko, Xu Xiaoping, Robert N. Willette

Publikováno v: American journal of physiology. Heart and circulatory physiology. 305(6)

Human-induced pluripotent stem cell-derived cardiomyocytes (hiPS-CMs) have been recently derived and are used for basic research, cardiotoxicity assessment, and phenotypic screening. However, the hiPS-CM phenotype is dependent on their derivation, ag

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0dcf66c81cf63f4f12ecb74a266da51c
https://pubmed.ncbi.nlm.nih.gov/23832699

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Improving the developability profile of pyrrolidine progesterone receptor partial agonists

Publikováno v: Bioorganicmedicinal chemistry letters. 20(1)

The previously reported pyrrolidine class of progesterone receptor partial agonists demonstrated excellent potency but suffered from serious liabilities including hERG blockade and high volume of distribution in the rat. The basic pyrrolidine amine w

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1c93d4e9e72254132d06ddbc41c09457
https://pubmed.ncbi.nlm.nih.gov/19926282

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Estrogen-induced stromal cell-derived factor-1 (SDF-1/Cxcl12) expression is repressed by progesterone and by Selective Estrogen Receptor Modulators via estrogen receptor alpha in rat uterine cells and tissues

Autor: Jeffrey D. Bray, Qi Wang, Ryan J. Boyle, Nicholas J. Laping, Eugene T. Grygielko, Lindsay Glace, Anthony C. Sulpizio

Publikováno v: Steroids. 74(13-14)

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 uterine origins, endometriotic lesions and resulting symptoms are

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::59360e1656489fb0e2f7cc3a06c321ec
https://pubmed.ncbi.nlm.nih.gov/19665469

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Rational design of orally-active, pyrrolidine-based progesterone receptor partial agonists

Autor: Eugene T. Grygielko, Shawn P. Williams, Lindsay E. Glace, Jeffrey D. Bray, Chaya Duraiswami, James S. Frazee, Kevin P. Madauss, David G. Washburn, Tram H. Hoang, Leahann Lapinski, Walter Trizna, Nicholas J. Laping, Scott K. Thompson

Publikováno v: Bioorganicmedicinal chemistry letters. 19(16)

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 agonist class containing a pyrrolidine ring was designed. Members of this class of N-alkylpyrroli

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6097498d950430c3690a93280e236dee
https://pubmed.ncbi.nlm.nih.gov/19595590

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