Literature DB >> 12565954

Synthesis and SAR of alpha-acylaminoketone ligands for control of gene expression.

Colin M Tice1, Robert E Hormann, Christine S Thompson, Jennifer L Friz, Caitlin K Cavanaugh, Enrique L Michelotti, Javier Garcia, Ernesto Nicolas, Fernando Albericio.   

Abstract

A lead discovery library and a follow-up focused library of alpha-acylaminoketones were designed based on known dibenzoylhydrazine ecdysone agonists, including GS(TM)-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 alpha-acylaminoketones were comparable to GS(TM)-E in this assay.

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Year:  2003        PMID: 12565954     DOI: 10.1016/s0960-894x(02)00980-0

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  5 in total

Review 1.  Insect cell culture and applications to research and pest management.

Authors:  Guy Smagghe; Cynthia L Goodman; David Stanley
Journal:  In Vitro Cell Dev Biol Anim       Date:  2009-02-27       Impact factor: 2.416

2.  In Silico Identification of Chemicals Capable of Binding to the Ecdysone Receptor.

Authors:  Claire L Mellor; Knut Erik Tollefsen; Carlie LaLone; Mark T D Cronin; James W Firman
Journal:  Environ Toxicol Chem       Date:  2020-06-04       Impact factor: 4.218

Review 3.  Practical uses for ecdysteroids in mammals including humans: an update.

Authors:  R Lafont; L Dinan
Journal:  J Insect Sci       Date:  2003       Impact factor: 1.857

4.  Nonsteroidal ecdysone receptor agonists use a water channel for binding to the ecdysone receptor complex EcR/USP.

Authors:  Christopher Browning; Alastair G McEwen; Kotaro Mori; Taiyo Yokoi; Dino Moras; Yoshiaki Nakagawa; Isabelle M L Billas
Journal:  J Pestic Sci       Date:  2021-02-20       Impact factor: 2.529

5.  Reporter gene assays for screening and identification of novel molting hormone- and juvenile hormone-like chemicals.

Authors:  Sayoko Ito-Harashima; Takashi Yagi
Journal:  J Pestic Sci       Date:  2021-02-20       Impact factor: 2.529

  5 in total

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