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pubmed-article:3127825pubmed:abstractTextThe 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.lld:pubmed
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pubmed-article:3127825pubmed:issn0027-8424lld:pubmed
pubmed-article:3127825pubmed:authorpubmed-author:LeeS SSSlld:pubmed
pubmed-article:3127825pubmed:authorpubmed-author:NakanishiKKlld:pubmed
pubmed-article:3127825pubmed:authorpubmed-author:CherbasPPlld:pubmed
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pubmed-article:3127825pubmed:volume85lld:pubmed
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pubmed-article:3127825pubmed:pagination2096-100lld:pubmed
pubmed-article:3127825pubmed:dateRevised2010-9-9lld:pubmed
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pubmed-article:3127825pubmed:articleTitle26-[125I]iodoponasterone A is a potent ecdysone and a sensitive radioligand for ecdysone receptors.lld:pubmed
pubmed-article:3127825pubmed:affiliationDepartment of Biology, Indiana University, Bloomington 47405.lld:pubmed
pubmed-article:3127825pubmed:publicationTypeJournal Articlelld:pubmed
pubmed-article:3127825pubmed:publicationTypeResearch Support, U.S. Gov't, P.H.S.lld:pubmed
pubmed-article:3127825pubmed:publicationTypeResearch Support, Non-U.S. Gov'tlld:pubmed
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