On June 30, 2021, Mayasich, Sally A.; Korte, Joseph J.; Denny, Jeffrey S.; Hartig, Phillip C.; Olker, Jennifer H.; DeGoey, Philip; O’Flanagan, Joseph; Degitz, Sigmund J.; Hornung, Michael W. published an article.Electric Literature of 96-76-4 The title of the article was Xenopus laevis and human type 3 iodothyronine deiodinase enzyme cross-species sensitivity to inhibition by ToxCast chemicals. And the article contained the following:
Deiodinase enzymes are critical for tissue-specific and temporal control of activation or inactivation of thyroid hormones during vertebrate development, including amphibian metamorphosis. We previously screened ToxCast chems. for inhibitory activity toward human recombinant Type 3 iodothyronine deiodinase enzyme (hDIO3) and subsequently produced Xenopus laevis recombinant dio3 enzyme (Xldio3) with the goals to identify specific chem. inhibitors of Xldio3, to evaluate cross-species sensitivity and explore whether the human assay results are predictive of the amphibian. We identified a subset of 356 chems. screened against hDIO3 to test against Xldio3, initially at a single concentration (200μM), and further tested 79 in concentration-response mode. Most chems. had IC50 values lower for hDIO3 than for Xldio3 and many had steep Hill slopes (a potential indication of non-specific inhibition). However, eight of the most potent chems. are likely specific inhibitors, with IC50 values of 14μM or less, Hill slopes near -1 and curves not significantly different between species likely due to conservation of catalytically active amino acids. Controlling for assay conditions, human in vitro screening results can be predictive of activity in the amphibian assay. This study lays the groundwork for future studies using recombinant non-mammalian proteins to test cross-species sensitivity to chems. The views expressed in this paper are those of the authors and do not necessarily reflect the views or policies of the U. The experimental process involved the reaction of 2,4-Di-tert-butylphenol(cas: 96-76-4).Electric Literature of 96-76-4
The Article related to xenopus human iodothyronine deiodinase screening endocrine disruptor, deiodinase, endocrine disruption, screening, thyroid, xenopus laevis, Toxicology: Methods (Including Analysis) and other aspects.Electric Literature of 96-76-4
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