Výsledky vyhledávání - "Chii Whei Hu"

Discovery of N-[5-(6-Chloro-3-cyano-1-methyl-1H-indol-2-yl)-pyridin-3-ylmethyl]-ethanesulfonamide, a Cortisol-Sparing CYP11B2 Inhibitor that Lowers Aldosterone in Human Subjects

Autor: Dean F. Rigel, Kerry S. Russell, Lu Gan, Julien Papillon, Chii-Whei Hu, Changgang Lou, Alok K. Singh, Daniel LaSala, Wei Chen, Gary Michael Ksander, Fumin Fu, Catherine Watson, Jennifer Leung-Chu, Arco Y. Jeng, Christopher M. Adams, Guiqing Liang, John A. Vest, Michael E. Beil

Publikováno v: Journal of Medicinal Chemistry. 58:9382-9394

Human clinical studies conducted with LCI699 established aldosterone synthase (CYP11B2) inhibition as a promising novel mechanism to lower arterial blood pressure. However, LCI699's low CYP11B1/CYP11B2 selectivity resulted in blunting of adrenocortic

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c1e6c50d8e5e31a37972d238e9fe1c8c
https://doi.org/10.1021/acs.jmedchem.5b01545

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The discovery of potent inhibitors of aldosterone synthase that exhibit selectivity over 11-β-hydroxylase

Autor: Qian Liu, Chun Zhang, Chang Rao, Jie Shi, Dean F. Rigel, Gary Michael Ksander, Chii-Whei Hu, Clayton Springer, Sherri Smith, Jennifer Leung-Chu, Guiqing Liang, Erik Meredith, Rajeshri Ganesh Karki, Dan LaSala, Arco Y. Jeng, Christopher M. Adams

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 20:4324-4327

Aldosterone, the final component of the renin-angiotensin-aldosterone system, plays an important role in the pathophysiology of hypertension and congestive heart failure. Aldosterone synthase (CYP11B2) catalyzes the last three steps of aldosterone bi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::592c3e259c3039f3b88071d2f84281a6
https://doi.org/10.1016/j.bmcl.2010.06.086

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Structure-Activity Relationships, Pharmacokinetics, and in Vivo Activity of CYP11B2 and CYP11B1 Inhibitors

Publikováno v: Journal of medicinal chemistry. 58(11)

CYP11B2, the aldosterone synthase, and CYP11B1, the cortisol synthase, are two highly homologous enzymes implicated in a range of cardiovascular and metabolic diseases. We have previously reported the discovery of LCI699, a dual CYP11B2 and CYP11B1 i

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::0ae31b3435b92f18b555f524e3460454
https://pubmed.ncbi.nlm.nih.gov/25953419

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Synergistic Stimulation of Aldosterone Production in Human Adrenocortical Carcinoma NCI-H295R Cells by Endothelin-1 and Angiotensin II

Autor: Chii-Whei Hu, Randy Lee Webb, Arco Y. Jeng

Publikováno v: Journal of Cardiovascular Pharmacology. 44:S289-S292

Aldosterone has recently been implicated in the pathogenesis of heart failure. The purpose of the present study was to determine the effect of endothelin-1 (ET-1) and angiotensin II (Ang II), two potent vasoconstrictors that are also involved in hear

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::5a21310f47615da6d6fbcb2918cb9739
https://doi.org/10.1097/01.fjc.0000166276.32421.1d

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Aldosterone synthase inhibition: cardiorenal protection in animal disease models and translation of hormonal effects to human subjects

Autor: Catherine Watson, Dean F. Rigel, Daniel LaSala, Fumin Fu, Michael E. Beil, Sam Rebello, Arco Y. Jeng, Jing Liu, Chii-Whei Hu, William P. Dole, Yiming Zhang, Joël Ménard, Jennifer Leung-Chu, Wei Chen, Guiqing Liang

Publikováno v: Journal of Translational Medicine
Journal of Translational Medicine, BioMed Central, 2014, 12 (1), pp.340

Background Aldosterone synthase inhibition provides the potential to attenuate both the mineralocorticoid receptor-dependent and independent actions of aldosterone. In vitro studies with recombinant human enzymes showed LCI699 to be a potent, reversi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2d5ec08ea895494190151feb67d25b61
http://europepmc.org/articles/PMC4301837

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The in vitro and ex vivo antioxidant properties, and hypolipidemic activity of CGP 2881

Autor: David Louis Feldman, W.Kit Sawyer, Kenneth S. Leonards, Michael Jeune, Chii-Whei Hu, Robin Sharif, Therese C Mogelesky, Margaret F. Prescott

Publikováno v: Atherosclerosis. 144:343-355

This report describes the in vitro and ex vivo antioxidant properties of a new antioxidant, CGP 2881. This compound is structurally similar to probucol, in that both compounds contain bis-tertiary butyl phenyl groups. However, CGP 2881 consistently i

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::cfe68be597f6ef2b8e26aa7606225f23
https://doi.org/10.1016/s0021-9150(99)00002-7

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Discovery and in Vivo Evaluation of Potent Dual CYP11B2 (Aldosterone Synthase) and CYP11B1 Inhibitors

Autor: Erik Meredith, Michael Paul Capparelli, Gary Michael Ksander, Chang Rao, Robin Burgis, Julien Papillon, Lauren G. Monovich, Dean F. Rigel, Alok K. Singh, Arco Y. Jeng, Chii-Whei Hu, Karl Miranda, Daniel LaSala, Qian Liu, Fumin Fu, Michael E. Beil, Qi-Ying Hu, Patrick J. Morris

Publikováno v: ACS medicinal chemistry letters. 4(12)

Aldosterone is a key signaling component of the renin-angiotensin-aldosterone system and as such has been shown to contribute to cardiovascular pathology such as hypertension and heart failure. Aldosterone synthase (CYP11B2) is responsible for the fi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::24dde8962d19a1a500167875ed7ff669
https://pubmed.ncbi.nlm.nih.gov/24900631

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Demonstration of potent lipid-lowering activity by a thyromimetic agent devoid of cardiovascular and thermogenic effects

Autor: Kenneth S. Leonards, Steele Ronald Edward, Jong M. Wasvary, E.C. Yurachek, Zouhair F. Stephan, Chii Whei Hu, Robin Sharif, Thomas H. Hintze

Publikováno v: Atherosclerosis. 126:53-63

A potent lipid-lowering thyromimetic (CGS 26214) devoid of cardiac and thermogenic activity was identified based on its ability to preferentially access and bind the nuclear fraction of hepatocytes over that of myocytes in culture. The difference in

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ad869be437aa034f8ff34a204dda59eb
https://doi.org/10.1016/0021-9150(96)05893-5

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Pharmacodynamic and pharmacokinetic characterization of the aldosterone synthase inhibitor FAD286 in two rodent models of hyperaldosteronism: comparison with the 11beta-hydroxylase inhibitor metyrapone

Autor: Arco Y. Jeng, Dean F. Rigel, Guiqing Liang, Michael E. Beil, Fumin Fu, Chii-Whei Hu

Publikováno v: The Journal of pharmacology and experimental therapeutics. 334(1)

Aldosterone synthase (CYP11B2) inhibitors (ASIs) represent an attractive therapeutic approach for mitigating the untoward effects of aldosterone. We characterized the pharmacokinetic/pharmacodynamic relationships of a prototypical ASI, (+)-(5R)-4-(5,

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9a5bdbe2d5ccb2a5b1d0ef1c318d096e
https://pubmed.ncbi.nlm.nih.gov/20354176

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