Nuclear Hormone Receptor Screening in Drug Discovery

2016 ◽  
pp. 203-227
Keyword(s):  
Drug Discovery ◽  
Hormone Receptor ◽  
Nuclear Hormone Receptor

Coactivators in Assay Design for Nuclear Hormone Receptor Drug Discovery

2003 ◽  
Vol 1 (6) ◽  
pp. 835-842 ◽  
Author(s):  
Taosheng Chen ◽  
Wen Xie ◽  
Michele Agler ◽  
Martyn Banks
Keyword(s):  
Drug Discovery ◽  
Hormone Receptor ◽  
Nuclear Hormone Receptor ◽  
Assay Design

scholarly journals Phosphorylation of the Hinge Domain of the Nuclear Hormone Receptor LRH-1 Stimulates Transactivation

2006 ◽  
Vol 281 (12) ◽  
pp. 7850-7855 ◽  
Author(s):  
Yoon-Kwang Lee ◽  
Yun-Hee Choi ◽  
Steven Chua ◽  
Young Joo Park ◽  
David D. Moore
Keyword(s):  
Hormone Receptor ◽  
Nuclear Hormone Receptor ◽  
Hinge Domain

scholarly journals Pseudoginsenoside F11, a Novel Partial PPARγAgonist, Promotes Adiponectin Oligomerization and Secretion in 3T3-L1 Adipocytes

PPAR Research ◽  
2013 ◽  
Vol 2013 ◽  
pp. 1-8 ◽  
Author(s):  
Guoyu Wu ◽  
Junyang Yi ◽  
Ling Liu ◽  
Pengcheng Wang ◽  
Zhijie Zhang ◽  
...  
Keyword(s):  
Type 2 Diabetes ◽  
Side Effects ◽  
Hormone Receptor ◽  
Adipocyte Differentiation ◽  
American Ginseng ◽  
Nuclear Hormone Receptor ◽  
Targeted Therapeutics ◽  
Panax Quinquefolium ◽  
Master Regulator

PPARγis a nuclear hormone receptor that functions as a master regulator of adipocyte differentiation and development. Full PPARγagonists, such as the thiazolidinediones (TZDs), have been widely used to treat type 2 diabetes. However, they are characterized by undesirable side effects due to their strong agonist activities. Pseudoginsenoside F11 (p-F11) is an ocotillol-type ginsenoside isolated fromPanax quinquefolium L.(American ginseng). In this study, we found that p-F11 activates PPARγwith modest adipogenic activity. In addition, p-F11 promotes adiponectin oligomerization and secretion in 3T3-L1 adipocytes. We also found that p-F11 inhibits obesity-linked phosphorylation of PPARγat Ser-273 by Cdk5. Therefore, p-F11 is a novel partial PPARγagonist, which might have the potential to be developed as a new PPARγ-targeted therapeutics for type 2 diabetes.

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