551964-10-4Relevant articles and documents
Ketone ligands for modulating the expression of exogenous genes via an ecdysone receptor complex
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Page 34, (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:
Synthesis and SAR of α-acylaminoketone ligands for control of gene expression
Tice, Colin M.,Hormann, Robert E.,Thompson, Christine S.,Friz, Jennifer L.,Cavanaugh, Caitlin K.,Michelotti, Enrique L.,Garcia, Javier,Nicolas, Ernesto,Albericio, Fernando
, p. 475 - 478 (2007/10/03)
A lead discovery library and a follow-up focused library of α-acylaminoketones were designed based on known dibenzoylhydrazine ecdysone agonists, including GS-E. The compounds were assayed in mammalian cells expressing the ecdysone receptor from Bombyx mori for their ability to cause expression of a reporter gene downstream of an ecdysone response element. The most potent α-acylaminoketones were comparable to GS-E in this assay.