Effects of thiocyanate on cytosol androgen receptor from Shionogi carcinoma 115.
The effects of KSCN and other chaotropic salts on the androgen receptor in cytosol of Shionogi carcinoma 115 were studied by means of charcoal adsorption assay and sucrose gradient centrifugation. When KSCN or NaSCN was added to the [3H]-dihydrotestosterone-cytosol mixture at the final concentration of 0.5 M, the androgen binding to the cytosol receptor was considerably inhibited. The inhibition reached maximum within 5 h at 0 degrees C and was dependent on the kind of chaotropic anion added: the potency of inhibitory effect in descending order was KSCN greater than KI greater than KBr greater than KCl. The inhibition was not observed in the estradiol-receptor interaction with KSCN or NaSCN up to 0.5 M. When 0.5 M KSCN-treated androgen-cytosol mixture was subjected to gel filtration or (NH4)2SO4 fractionation to remove the salt, a partial recovery (30-40%) in specific binding activity was observed. The binding activity of androgen receptor was unaffected by a treatment with KSCN up to 0.1 M and the androgen-receptor complex sedimented in a 5S form in 0.1-0.3 M KSCN, 0.5 M KCl or 0.5 M KBr. These results suggest that the binding activity of androgen receptor is more susceptible than that of estrogen receptor to chaotropic salts which cause impairment in intramolecular hydrophobic interactions.
D000230:Adenocarcinoma / Q000378:metabolism*; D000818:Animals; D001965:Bromides / Q000494:pharmacology; D002499:Centrifugation, Density Gradient; D003600:Cytosol / Q000378:metabolism; D013196:Dihydrotestosterone / Q000378:metabolism; D008297:Male; D051379:Mice; D009374:Neoplasms, Experimental / Q000378:metabolism; D011188:Potassium / Q000494:pharmacology; D017680:Potassium Compounds; D011193:Potassium Iodide / Q000494:pharmacology; D011944:Receptors, Androgen / Q000187:drug effects / Q000378:metabolism*; D011987:Receptors, Steroid / Q000378:metabolism*; D013861:Thiocyanates / Q000494:pharmacology*
D001965:Bromides; D017680:Potassium Compounds; D011944:Receptors, Androgen; D011987:Receptors, Steroid; D013861:Thiocyanates; D013196:Dihydrotestosterone; D011193:Potassium Iodide; C039004:potassium bromide; D011188:Potassium; C009941:potassium thiocyanate