Article
Diuretic drug binding to human glutathione transferase P1-1: potential role of Cys-101 revealed in the double mutant C47S/Y108V.
Journal of molecular recognition : JMR - 1 Jan 2000
Quesada-Soriano Indalecio, Parker Lorien J, Primavera Alessandra, Wielens Jerome, Holien Jessica K, Casas-Solvas Juan M, Vargas-Berenguel Antonio, Aguilera Ana M, Nuccetelli Marzia, Mazzetti Anna P, Lo Bello Mario, Parker Michael W, García-Fuentes Luis
Abstract excerpt
The diuretic drug ethacrynic acid (EA), both an inhibitor and substrate of pi class glutathione S-transferase (GST P1-1), has been tested in clinical trials as an adjuvant in chemotherapy. We recently studied the role of the active site residue Tyr-108 in binding EA to the enzyme and found that the analysis was complicated by covalent binding of this drug to the highly reactive Cys-47. Previous attempts to...
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