Diethyl pyrocarbonate, a histidine selective reagent, inhibits estrogen binding to receptor protein in rat uterus cytosol.
We find that at pH 6.1 diethyl pyrocarbonate inhibits estrogen binding to its receptor protein in rat uterus. Hydroxylamine partially reverses this inhibition and estrogen partially protects its receptor protein from this inhibition. We suggest that the estrogen receptor protein in rat uterus contains a nucleophilic site that either overlaps or is near the estrogen binding site. Based on the pH of inhibition reaction, the receptor concentration in the experiment, and the partial reversal of the inhibition by hydroxylamine, we suggest that this site contains a histidine residue or possibly an unusually reactive tyrosine residue that is important for estrogen binding.
D000818:Animals; D001665:Binding Sites; D003600:Cytosol / Q000378:metabolism; D004047:Diethyl Pyrocarbonate / Q000494:pharmacology*; D004967:Estrogens / Q000378:metabolism*; D005260:Female; D005561:Formates / Q000494:pharmacology*; D006639:Histidine; D006863:Hydrogen-Ion Concentration; D066298:In Vitro Techniques; D051381:Rats; D011919:Rats, Inbred Strains; D011960:Receptors, Estrogen / Q000187:drug effects* / Q000378:metabolism; D014599:Uterus / Q000378:metabolism*
D004967:Estrogens; D005561:Formates; D011960:Receptors, Estrogen; D006639:Histidine; D004047:Diethyl Pyrocarbonate