NDLI: 26-[125I]iodoponasterone A is a potent ecdysone and a sensitive radioligand for ecdysone receptors.

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26-[125I]iodoponasterone A is a potent ecdysone and a sensitive radioligand for ecdysone receptors.

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26-[125I]iodoponasterone A is a potent ecdysone and a sensitive radioligand for ecdysone receptors.

Content Provider	World Health Organization (WHO)-Global Index Medicus
Author	Cherbas, L. Lee, S. S. Cherbas, P. Nakanishi, K.
Description	Author Affiliation: Cherbas P ( Department of Biology, Indiana University, Bloomington 47405.);
Abstract	The effects of ecdysone, the steroid molting hormone of arthropods, are of considerable interest both to insect physiologists and to those studying steroid-regulated gene expression. Yet progress in understanding ecdysone receptors has been inhibited by the lack of a suitable highly radioactive hormone analog with high affinity for the receptor. Here we report that the synthetic ecdysteroid 26-iodoponasterone A is one of the most active ecdysones known, inducing half-maximal morphological transformation in Drosophila Kc167 cells when present at 0.5 nM. 26-[125I]Iodoponasterone A can be prepared at a specific activity of 2175 Ci/mmol (1 Ci = 37 GBq) by reaction of the precursor 26-mesylinokosterone with carrier-free Na125I. The radiolabeled material binds to Kc167 cell ecdysone receptors specifically and with affinity (Kd ca. 3.8 X 10(-10) M). Thus, 26-[125I]iodoponasterone A appears to be a superior radioligand for ecdysone receptors on grounds both of affinity and of specific activity. Its ready availability should greatly facilitate studies of these receptors.
ISSN	00278424
e-ISSN	10916490
Journal	Proceedings of the National Academy of Sciences of the United States of America
Issue Number	7
Volume Number	85
Language	English
Publisher	National Academy of Sciences
Publisher Date	1988-05-01
Publisher Place	United States
Access Restriction	Open
Subject Keyword	Ecdysone Metabolism Ecdysterone Analogs & Derivatives Receptors, Steroid Animals Binding, Competitive Cell Line Drosophila Melanogaster Cytology Chemical Synthesis Pharmacology Research Support, Non-U.S. Gov't Research Support, U.S. Gov't, P.H.S. Multidisciplinary
Content Type	Text
Resource Type	Article
Subject	Multidisciplinary

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