644980-60-9Relevant academic research and scientific papers
Ketone ligands for modulating the expression of exogenous genes via an ecdysone receptor complex
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Page 32, (2008/06/13)
This invention relates to a method to modulate exogenous gene expression in which an ecdysone receptor complex comprising: a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising:
Optimization of α-acylaminoketone ecdysone agonists for control of gene expression
Tice, Colin M.,Hormann, Robert E.,Thompson, Christine S.,Friz, Jennifer L.,Cavanaugh, Caitlin K.,Saggers, Jessica A.
, p. 1883 - 1886 (2007/10/03)
Fifteen new α-acylaminoketones were prepared by four different routes in an initial effort to optimize the potency of these compounds as ecdysone agonists. The compounds were assayed in mammalian cells expressing the ecdysone receptors from Bombyx mori (BmEcR) and Choristoneura fumiferana (CfEcR) for their ability to cause expression of a reporter gene downstream of an ecdysone response element. A new α-acylaminoketone was identified which had activity equal to that of the standard dibenzoylhydrazine ecdysone agonist GS-E in the assay based on CfEcR.
