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Reversible conjugation of ethacrynic acid with glutathione and human glutathione S-transferase P1-1.
Cancer research, no. 4 (1994): 915-919
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resulting in a completely different time course for the inhibition.howeverthese findings may have several implications. under normal physi- ological conditions the inhibition of gst pi-1 by covalent binding of ea would be reversed by glutathionewhen glutathione levels are low the covalent inhibi- tion might be predominantleaving reversible inhibition by the glutathione conjugate of ea and by ea itself as the main mechanism of inhibition更多(5+)
摘要
The reversibility of the conjugation reaction of the diuretic drug ethacrynic acid (EA), an alpha,beta-unsaturated ketone, with glutathione and glutathione S-transferase P1-1 (GST P1-1) has been studied. When the glutathione conjugate of EA was incubated with a 5-fold molar excess of N-acetyl-L-cysteine or GST P1-1, a time-dependent trans...更多
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