Výsledky vyhledávání - "Jessica D. Dietz"

Discovery of Novel Cyanodihydropyridines as Potent Mineralocorticoid Receptor Antagonists

Autor: Kaliappan Iyanar, Jessica D. Dietz, Graciela B. Arhancet, Horng-Chih Huang, Danny J. Garland, Marcia I. Heron, Silvia I. Pomposiello, Xiao Hu, Len F. Lee, Joe T. Collins, Scott S. Woodard, James Robert Blinn, Maria A. Payne, Brenda L. Case, Rhonda S. Woerndle

Publikováno v: Journal of Medicinal Chemistry. 53:5970-5978

A new 1,4-dihydropyridine 5a, containing a cyano group at the C3 position, was recently reported to possess excellent mineralocorticoid receptor (MR) antagonist in vitro potency and no calcium channel-blocker (CCB) activity. In the present study, we

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9288e4053ed7e7f775bce265c4ec3184
https://doi.org/10.1021/jm100506y

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Stereochemical Requirements for the Mineralocorticoid Receptor Antagonist Activity of Dihydropyridines

Autor: Grace M. Wagner, Joe T. Collins, Scott S. Woodard, Randal E Numann, Kaliappan Iyanar, Graciela B. Arhancet, Danny J. Garland, James Robert Blinn, Jessica D. Dietz, Horng-Chih Huang, Xiao Hu

Publikováno v: Journal of Medicinal Chemistry. 53:4300-4304

A number of known 1,4-dihydropyridine CCBs were identified as having comparable potency to the steroidal MR antagonist eplerenone. Chiral resolution of mebudipine revealed that MR and CCB activity reside in opposite enantiomers. Small molecule X-ray

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f6e7af97f6c33d3bb740cfc75d288cac
https://doi.org/10.1021/jm1002827

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The Ligand-Dependent Interaction of Mineralocorticoid Receptor with Coactivator and Corepressor Peptides Suggests Multiple Activation Mechanisms

Autor: Nataliia V. Krasnoperova, Suzhen Li, Xiao Hu, Monica L. Hultman, Sarah Du, Jessica D. Dietz, Dean Welsch, Deepak S. Lala, Chunsheng Xia

Publikováno v: Molecular Endocrinology. 19:1460-1473

We investigated the coregulator (coactivator and corepressor) interactions with the mineralocorticoid receptor (MR) that lead to activation and inhibition of the receptor in the presence of agonist and/or antagonist. Our results indicate that MR liga

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f9d145cc1f59a0457e15fe116c2b1200
https://doi.org/10.1210/me.2004-0537

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Repression of p65 Transcriptional Activation by the Glucocorticoid Receptor in the Absence of Receptor-Coactivator Interactions

Autor: Jun Wu, Yu Li, Jessica D. Dietz, Deepak S. Lala

Publikováno v: Molecular Endocrinology. 18:53-62

Glucocorticoids are among the most potent antiinflammatory agents, acting through the glucocorticoid receptor (GR) to suppress gene expression of a variety of cytokines. This appears to be via transcriptional interference (or transrepression) of key

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::95efe2b2b2a26061c0532be98b920728
https://doi.org/10.1210/me.2002-0373

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The antagonists but not partial agonists of glucocorticoid receptor ligands show substantial side effect dissociation

Autor: Cansu Tunca, Xiao Hu, Sarah Du, Elizabeth G. Webb, Susan Hummert, Jessica D. Dietz, Jamie Lee, Timothy Braden, Sharon Rouw, R. Keith Webber, Shridhar Hegde, Kelly R. Long, Mark Gerard Obukowicz

Publikováno v: Endocrinology. 152(8)

A synthetic glucocorticoid receptor (GR) ligand with the efficacy of a glucocorticoid, but without the accompanying side effects, would meet an unmet medical need for the treatment of inflammatory diseases. It was hypothesized that a GR ligand that s

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::a7c5449cd13422d008ef4407c998eb9a
https://pubmed.ncbi.nlm.nih.gov/21785014

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Torcetrapib induces aldosterone and cortisol production by an intracellular calcium-mediated mechanism independently of cholesteryl ester transfer protein inhibition

Autor: Andrew H. Smith, Jessica D. Dietz, Chunsheng Xia, Haodan Yuan, Delvin R. Knight, David Austen Perry, Joan A. Keiser, Xiao Hu, William T. Loging

Publikováno v: Endocrinology. 150(5)

ILLUMINATE (Investigation of Lipid Level Management to Understand its Impact in Atherosclerotic Events), the phase 3 morbidity and mortality trial of torcetrapib, a cholesteryl ester transfer protein (CETP) inhibitor, identified previously undescribe

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::572658652789b516a968fd28ebaadc5f
https://pubmed.ncbi.nlm.nih.gov/19383878

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A number of marketed dihydropyridine calcium channel blockers have mineralocorticoid receptor antagonist activity

Autor: Jessica D. Dietz, James Robert Blinn, Maria A. Payne, Chunsheng Xia, Sarah Du, John W. Funder, Charles W. Bolten, Xiao Hu

Publikováno v: Hypertension (Dallas, Tex. : 1979). 51(3)

Calcium channel blockers are widely used antihypertensives. Mineralocorticoid receptor antagonists are also used to treat hypertension and heart failure. We report here that a number of widely used dihydropyridine class calcium channel blockers are a

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::fa2b95c7e9d7bde69d4f558108e75417
https://pubmed.ncbi.nlm.nih.gov/18250364

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