Eugene T Grygielko
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Explore the profile of Eugene T Grygielko including associated specialties, affiliations and a list of published articles.
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13
Citations
284
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Recent Articles
1.
Ivashchenko C, Pipes G, Lozinskaya I, Lin Z, Xiaoping X, Needle S, et al.
Am J Physiol Heart Circ Physiol
. 2013 Jul;
305(6):H913-22.
PMID: 23832699
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,...
2.
Kallander L, Washburn D, Hoang T, Frazee J, Stoy P, Johnson L, et al.
Bioorg Med Chem Lett
. 2009 Nov;
20(1):371-4.
PMID: 19926282
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...
3.
Glace L, Grygielko E, Boyle R, Wang Q, Laping N, Sulpizio A, et al.
Steroids
. 2009 Aug;
74(13-14):1015-24.
PMID: 19665469
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...
4.
Wang Y, Duraiswami C, Madauss K, Tran T, Williams S, Deng S, et al.
Bioorg Med Chem Lett
. 2009 Aug;
19(17):4916-9.
PMID: 19664922
High throughput screening of the corporate compound collection led to the identification of 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 as selective PR agonists. Initial SAR exploration leading to potent and...
5.
Washburn D, Hoang T, Frazee J, Johnson L, Hammond M, Manns S, et al.
Bioorg Med Chem Lett
. 2009 Jul;
19(16):4664-8.
PMID: 19616429
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...
6.
Thompson S, Washburn D, Frazee J, Madauss K, Hoang T, Lapinski L, et al.
Bioorg Med Chem Lett
. 2009 Jul;
19(16):4777-80.
PMID: 19595590
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...
7.
Synthesis and SAR of amino acid-derived heterocyclic progesterone receptor full and partial agonists
Hammond M, Patterson J, Manns S, Hoang T, Washburn D, Trizna W, et al.
Bioorg Med Chem Lett
. 2009 Apr;
19(10):2637-41.
PMID: 19376703
Two classes of amino acid-derived heterocyclic progesterone receptor ligands were developed to address the metabolic issues posed by the dimethyl amide functionality of the lead compound (1). The tetrazole-derived ligands...
8.
Madauss K, Grygielko E, Deng S, Sulpizio A, Stanley T, Wu C, et al.
Mol Endocrinol
. 2007 Mar;
21(5):1066-81.
PMID: 17356170
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...
9.
Gellibert F, de Gouville A, Woolven J, Mathews N, Nguyen V, Bertho-Ruault C, et al.
J Med Chem
. 2006 Mar;
49(7):2210-21.
PMID: 16570917
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...
10.
Grygielko E, Martin W, Tweed C, Thornton P, Harling J, Brooks D, et al.
J Pharmacol Exp Ther
. 2005 Mar;
313(3):943-51.
PMID: 15769863
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-beta1 (TGF-beta1) receptor, activin receptor-like kinase (ALK5). The compound inhibited ALK5 kinase activity with an...