Inhibition of nuclear uptake of glucocorticoid-receptor complex by aurintricarboxylic acid.
The presence of 50-200 microM aurintricarboxylic acid (ATA) blocked the uptake of [3H]-triamcinolone acetonide (3H-TA)-receptor complex from rat liver cytosol by isolated nuclei. The half-maximal inhibition (I.D.50) in the nuclear uptake of [3H]-TA-receptor complex was observed at 70- and 80 microM ATA depending upon whether the inhibitor was added prior to or following receptor activation. In addition, the nuclear-bound [3H]-TA-receptor complex from control samples could be completely extracted by an incubation with 20-100 microM ATA. The amount of [3H]-TA-receptor complex remained unchanged under these conditions. The effects of ATA may result due to its interaction with the glucocorticoid receptor at/near the sites that are involved in its nuclear uptake. ATA, therefore is a potentially useful chemical probe for analysis of glucocorticoid receptor.
D000315:Adrenalectomy; D000818:Animals; D001312:Aurintricarboxylic Acid / Q000494:pharmacology*; D002467:Cell Nucleus / Q000187:drug effects / Q000378:metabolism*; D003509:Cyclohexanecarboxylic Acids / Q000494:pharmacology*; D003600:Cytosol / Q000378:metabolism; D007700:Kinetics; D008099:Liver / Q000378:metabolism*; D008297:Male; D051381:Rats; D011919:Rats, Inbred Strains; D011965:Receptors, Glucocorticoid / Q000378:metabolism*; D011987:Receptors, Steroid / Q000378:metabolism*; D014222:Triamcinolone Acetonide / Q000378:metabolism*
D003509:Cyclohexanecarboxylic Acids; D011965:Receptors, Glucocorticoid; D011987:Receptors, Steroid; D001312:Aurintricarboxylic Acid; D014222:Triamcinolone Acetonide