To elucidate tetraiodothyronine (T4) metabolism in developing rat retina 5-monodeiodinating and 5'-monodeiodinating activities were studied. T4 was incubated with aliquots of homogenate or crude primary subcellular fractions, and the 3,3',5'-triiodothyronine (rT3) or 3,5,3'-triiodothyronine (T3) produced were measured by radioimmunoassay. Reaction rates were dependent on incubation time, tissue amount, temperature and pH. The optimum pH values were 7.8 and 7.2 respectively for rT3-forming and T3-forming systems. Conversion of T4 to either T3 or rT3 was dependent on dithiothreitol concentration, and the T4-5'-deiodinating activity was inhibited by propylthiouracil. Deiodinase activities were mainly found in the crude microsomes. The retinal 5'-monodeiodination rate of T4 was immeasurably low by the 2nd day and the highest values were reached on 15th day of postnatal development. On the other hand deiodination of the T4 tyrosyl ring shows a progressive decline from birth, and adult values were reached on the 15th day. Data support the hypothesis that, in developing rat thyroxine, phenolic and tyrosyl-ring deiodinase activities are present in the retina and their reciprocal changes may regulate morphological and biochemical cell maturation.
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http://dx.doi.org/10.1111/j.1432-1033.1984.tb08244.x | DOI Listing |
Mol Omics
December 2024
Department of Chemistry and Biochemistry, University of Texas at Arlington, Box 19065, 700 Planetarium Place, Room 130, Arlington, TX 76019, USA.
Designing reagents for protein labeling is crucial for investigating cellular events and developing new therapeutics. Historically, much effort has been focused on labeling lysine and arginine residues due to their abundance on the protein periphery. The chemo-selectivity of these reagents is a challenging yet crucial parameter for deciphering properties specifically associated with the targeted amino acid.
View Article and Find Full Text PDFChem Sci
August 2024
The University of Queensland, School of Biomedical Sciences Brisbane QLD 4072 Australia
Eur J Med Chem
October 2024
Perm Federal Scientific Centre, Institute of Technical Chemistry UB RAS, Academician Korolev St. 3, 614013, Perm, Russia. Electronic address:
For the first time, a synthetic route for preparing lupane and oleanane derivatives with a hydrogenated furan ring as a cycle A of triterpene scaffold is described. Most of the synthesized compounds, furanoterpenoids and their synthetic intermediates, were non-toxic against the tested cancer and non-cancerous cell lines, and evinced significant inhibitory activity with IC 1.0-9.
View Article and Find Full Text PDFJ Med Chem
June 2024
Institute of Inorganic Chemistry, University of Vienna, Vienna A-1090, Austria.
Nucleic Acids Res
November 2023
CMBC, CNRS UMR9187, INSERM U1196, Institut Curie, PSL Research University, 91405 Orsay, France.
Apurinic/apyrimidinic (AP) sites, 5-formyluracil (fU) and 5-formylcytosine (fC) are abundant DNA modifications that share aldehyde-type reactivity. Here, we demonstrate that polyamines featuring at least one secondary 1,2-diamine fragment in combination with aromatic units form covalent DNA adducts upon reaction with AP sites (with concomitant cleavage of the AP strand), fU and, to a lesser extent, fC residues. Using small-molecule mimics of AP site and fU, we show that reaction of secondary 1,2-diamines with AP sites leads to the formation of unprecedented 3'-tetrahydrofuro[2,3,4-ef]-1,4-diazepane ('ribodiazepane') scaffold, whereas the reaction with fU produces cationic 2,3-dihydro-1,4-diazepinium adducts via uracil ring opening.
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