Optimization of α-acylaminoketone ecdysone agonists for control of gene expression
| Autor: | Colin M. Tice, Caitlin K. Cavanaugh, Robert Eugene Hormann, Jessica A. Saggers, Christine S. Thompson, Jennifer L. Friz |
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| Rok vydání: | 2003 |
| Předmět: |
Transcriptional Activation
Agonist Ecdysone Receptors Steroid medicine.drug_class Clinical Biochemistry Response element Pharmaceutical Science CHO Cells Biochemistry Bombycidae chemistry.chemical_compound Genes Reporter Bombyx mori Cricetinae Drug Discovery Gene expression medicine Potency Animals Receptor Molecular Biology Reporter gene Molecular Structure biology Organic Chemistry General Medicine Ketones Bombyx beta-Galactosidase biology.organism_classification Cell biology Lepidoptera Gene Expression Regulation chemistry Molecular Medicine Ecdysone receptor |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 13:1883-1886 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/s0960-894x(03)00315-9 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
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