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Science 22 July 1988:
Vol. 241. no. 4864, pp. 467 - 469
DOI: 10.1126/science.3393913
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Articles

Science, Vol 241, Issue 4864, 467-469
Copyright © 1988 by American Association for the Advancement of Science

articles

RH 5849, a nonsteroidal ecdysone agonist: effects on a Drosophila cell line

KD Wing

Research Labs, Rohm and Haas Co., Spring House, PA 19477.

The steroid molting hormone 20-hydroxyecdysone is the physiological inducer of molting and metamorphosis in insects. In ecdysone-sensitive Drosophila Kc cells, the insecticide RH 5849 (1,2-dibenzoyl-1-tert-butylhydrazine) mimics the action of 20-hydroxyecdysone by causing the formation of processes, an inhibition of cell proliferation, and induction of acetylcholinesterase. RH 5849 also competes with [3H]ponasterone A for high-affinity ecdysone receptor sites from Kc cell extracts. Resistant cell populations selected by growth in the continued presence of either RH 5849 or 20-hydroxyecdysone are insensitive to both compounds and exhibit a decreased titer of measurable ecdysone receptors. Although it is less potent than 20-hydroxyecdysone in both whole-cell and cell-free receptor assays, RH 5849 is the first nonsteroidal ecdysone agonist.


THIS ARTICLE HAS BEEN CITED BY OTHER ARTICLES:
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A single point mutation in ecdysone receptor leads to increased ligand specificity: Implications for gene switch applications.
M. B. Kumar, T. Fujimoto, D. W. Potter, Q. Deng, and S. R. Palli (2002)
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RH 5849, a Nonsteroidal Ecdysone Agonist: Effects on Larval Lepidoptera.
K. D. WING, R. A. SLAWECKI, and G. R. CARLSON (1988)
Science 241, 470-472
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Identification of ligands and coligands for the ecdysone-regulated gene switch.
E. Saez, M. C. Nelson, B. Eshelman, E. Banayo, A. Koder, G. J. Cho, and R. M. Evans (2000)
PNAS 97, 14512-14517
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Science. ISSN 0036-8075 (print), 1095-9203 (online)