A Pregnane X Receptor Agonist with Unique Species-Dependent Stereoselectivity and Its Implications in Drug Development

2005 ◽  
Vol 68 (2) ◽  
pp. 403-413 ◽  
Author(s):  
Ying Mu ◽  
Corey R. J. Stephenson ◽  
Christopher Kendall ◽  
Simrat P. S. Saini ◽  
David Toma ◽  
...  
Keyword(s):  
Drug Development ◽  
Receptor Agonist ◽  
Pregnane X Receptor ◽  
Unique Species

scholarly journals Pregnane X Receptor in Drug Development

10.5772/27753 ◽  
2011 ◽  
Author(s):  
Su Sien ◽  
Yue-Ming Wang ◽  
Sergio C. ◽  
Taosheng Che
Keyword(s):  
Drug Development ◽  
Pregnane X Receptor

scholarly journals Solomonsterol A, a Marine Pregnane-X-Receptor Agonist, Attenuates Inflammation and Immune Dysfunction in a Mouse Model of Arthritis

Marine Drugs ◽  
2013 ◽  
Vol 12 (1) ◽  
pp. 36-53 ◽  
Author(s):  
Andrea Mencarelli ◽  
Claudio D'Amore ◽  
Barbara Renga ◽  
Sabrina Cipriani ◽  
Adriana Carino ◽  
...  
Keyword(s):  
Mouse Model ◽  
Receptor Agonist ◽  
Pregnane X Receptor ◽  
Immune Dysfunction

Modification in the side chain of solomonsterol A: discovery of cholestan disulfate as a potent pregnane-X-receptor agonist

2012 ◽  
Vol 10 (31) ◽  
pp. 6350 ◽  
Author(s):  
Valentina Sepe ◽  
Raffaella Ummarino ◽  
Maria Valeria D'Auria ◽  
Gianluigi Lauro ◽  
Giuseppe Bifulco ◽  
...  
Keyword(s):  
Receptor Agonist ◽  
Pregnane X Receptor ◽  
Side Chain

Human pregnane X receptor: a novel target for anticancer drug development

2014 ◽  
Vol 19 (1) ◽  
pp. 63-70 ◽  
Author(s):  
Vijay Rathod ◽  
Sumit Jain ◽  
Prajwal Nandekar ◽  
Abhay T. Sangamwar
Keyword(s):  
Drug Development ◽  
Anticancer Drug ◽  
Pregnane X Receptor ◽  
Novel Target ◽  
Anticancer Drug Development

Pregnane X Receptor agonist Increases the Expression Levels of the Plasma Membrane Monoamine Transporter

2014 ◽  
Vol 22 (1) ◽  
pp. 19
Author(s):  
Sung Kweon Cho ◽  
Haejin Oh ◽  
Se Hyang Hong ◽  
Min Soo Park ◽  
Jae Yong Chung
Keyword(s):  
Plasma Membrane ◽  
Receptor Agonist ◽  
Pregnane X Receptor ◽  
Monoamine Transporter ◽  
Expression Levels

Total Synthesis and Pharmacological Characterization of Solomonsterol A, a Potent Marine Pregnane-X-Receptor Agonist Endowed with Anti-Inflammatory Activity

2011 ◽  
Vol 54 (13) ◽  
pp. 4590-4599 ◽  
Author(s):  
Valentina Sepe ◽  
Raffaella Ummarino ◽  
Maria Valeria D’Auria ◽  
Andrea Mencarelli ◽  
Claudio D’Amore ◽  
...  
Keyword(s):  
Total Synthesis ◽  
Receptor Agonist ◽  
Pregnane X Receptor ◽  
Inflammatory Activity ◽  
Pharmacological Characterization ◽  
Anti Inflammatory

scholarly journals Treatment of Cardiovascular Disease by Traditional Chinese Medicine against Pregnane X Receptor

2014 ◽  
Vol 2014 ◽  
pp. 1-17 ◽  
Author(s):  
Kuen-Bao Chen ◽  
Hsin-Yi Chen ◽  
Kuan-Chung Chen ◽  
Calvin Yu-Chian Chen
Keyword(s):  
Cardiovascular Disease ◽  
Drug Development ◽  
Circulatory System ◽  
Docking Simulation ◽  
Pregnane X Receptor ◽  
Md Simulations ◽  
Positive Control ◽  
Hazardous Substances ◽  
Lead Compounds ◽  
Circulatory System Diseases

Recently, cardiovascular disease, also known as loop circulatory system diseases or disorders, is one of the serious diseases including heart disease, stroke, atherosclerosis, myocardial infarction, hypertension, hypotension, and thrombosis. Human pregnane X receptor, PXR, plays a crucial role in exogenous and endobiotic metabolism for rabbit, rat, mouse, and human. The PXR activation can protect the blood vessels from damage of hazardous substances. In this study we aim to investigate the potent lead compounds as PXR receptor agonist against cardiovascular disease. To improve drug development of TCM compounds, we aim to investigate the potent lead compounds as PXR agonists from the TCM compounds in TCM Database@Taiwan. The top three TCM compounds, bis(4-hydroxybenzyl) ether mono-β-D-glucopyranoside (BEMG), ixerisoside, and tangshenoside II, have displayed higher potent binding affinities than the positive control, PNU-142721, in the docking simulation. After MD simulations, which can optimize the result of docking simulation and validate the stability of H-bonds between each ligand and PXR protein under dynamic conditions, top TCM compounds, BEMG and tangshenoside II, maintain most of interactions with PXR protein, which keep the ligand binding stable in the binding domain. Hence, we propose BEMG and tangshenoside II as potential lead compounds for further study in drug development process with the PXR protein.

The First Total Synthesis of Solomonsterol B, a Marine Pregnane X Receptor Agonist

2012 ◽  
Vol 2012 (27) ◽  
pp. 5187-5194 ◽  
Author(s):  
Valentina Sepe ◽  
Raffaella Ummarino ◽  
Maria Valeria D'Auria ◽  
Barbara Renga ◽  
Stefano Fiorucci ◽  
...  
Keyword(s):  
Total Synthesis ◽  
Receptor Agonist ◽  
Pregnane X Receptor
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