High-throughput screening of ecdysone agonists using a reporter gene assay followed by 3-D QSAR analysis of the molting hormonal activity

2006 ◽  
Vol 14 (4) ◽  
pp. 1143-1159 ◽  
Author(s):  
Craig E. Wheelock ◽  
Yoshiaki Nakagawa ◽  
Toshiyuki Harada ◽  
Nobuhiro Oikawa ◽  
Miki Akamatsu ◽  
...  
2009 ◽  
Vol 26 (3) ◽  
pp. 345-349 ◽  
Author(s):  
Yoshihiro Narusaka ◽  
Mari Narusaka ◽  
Hiroshi Abe ◽  
Nami Hosaka ◽  
Masatomo Kobayashi ◽  
...  

2005 ◽  
Vol 3 (4) ◽  
pp. 393-400 ◽  
Author(s):  
Xiaoqing Shi ◽  
Wei Zheng ◽  
Jonathan E. Schneeweis ◽  
Paul A. Fischer ◽  
Berta Strulovici ◽  
...  

2007 ◽  
Vol 103 (1) ◽  
pp. 133-140 ◽  
Author(s):  
G. De Pascale ◽  
C. Grigoriadou ◽  
D. Losi ◽  
I. Ciciliato ◽  
M. Sosio ◽  
...  

2011 ◽  
Vol 205 ◽  
pp. S161-S162
Author(s):  
D. Hernández-Moreno ◽  
J. Freitas ◽  
J.H.J. van den Berg ◽  
C. Craig-Veit ◽  
M.L. Goodson ◽  
...  

2005 ◽  
Vol 10 (5) ◽  
pp. 437-446 ◽  
Author(s):  
Toby C. Kent ◽  
Kevin S. J. Thompson ◽  
Louise H. Naylor

Multiple assay formats have been developed for the pharmacological characterization of G-protein-coupled receptors (GPCRs) and for screening orphan receptors. However, the increased pace of target identification and the rapid expansion of compound libraries present the need to develop novel assay formats capable of screeningmultipleGPCRs simultaneously. To address this need, the authors have developed a generic dual-reporter gene assay that can detect ligand activity at 2 GPCRs within the same assay. Two stableHEK293 cell lineswere generated expressing either a firefly ( Photinus) luciferase gene under the control ofmultiple cAMP-response elements (CREs) or a Renillaluciferase gene under the control ofmultiple 12-Otetradecanoylphorbol-13-acetate (TPA)-responsive elements (TREs). Coseeded reporter cells were used to assess ligandbinding activity at bothGβ s-and Gβ q-coupled receptors. By selectively coexpressing receptors with a chimeric G-protein, agonist activitywas assessed atGβ i/o-coupled receptors in combinationwith eitherGβ s-or Gβ q-coupled receptors. The dual-reporter gene assaywas shown to be capable of simultaneously performing duplexed screens for a variety of agonist and/or antagonist combinations. The data generated from the duplexed reporter assays were pharmacologically relevant, and Zβ factor analysis indicated the suitability of both agonist and antagonist screens for use in high-throughput screening.


2008 ◽  
Vol 3 (9-10) ◽  
pp. 1276-1279 ◽  
Author(s):  
Kamna Nanda ◽  
Mou Chatterjee ◽  
Ranjana Arya ◽  
Shohini Mukherjee ◽  
Kulvinder Singh Saini ◽  
...  

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