RETINOIDS INHIBIT MAMMALIAN GLUTATHIONE TRANSFERASES

被引:16
作者
KULKARNI, AA [1 ]
KULKARNI, AP [1 ]
机构
[1] UNIV S FLORIDA,COLL PUBL HLTH,DEPT ENVIRONM & OCCUPAT HLTH,FLORIDA TOXICOL RES CTR,TAMPA,FL 33612
关键词
GLUTATHIONE TRANSFERASES; INHIBITION; RETINOIDS; CANCER TREATMENT;
D O I
10.1016/0304-3835(95)03749-M
中图分类号
R73 [肿瘤学];
学科分类号
100214 ;
摘要
Affinity-purified cytosolic glutathione transferases from adult female rat liver, adult human liver and human term placenta were used. Of the 8 retinoids tested, all-trans retinoic acid was found to be the most potent inhibitor of placental glutathione transferase. The inhibition was non-competitive and exhibited K-i values of 20 and 41 mu M for all-trans retinoic acid in the presence of varying concentrations of 1-chloro-2,4-dinitrobenzene and glutathione, respectively. Micromolar all-trans retinoic acid also caused significant (30-90%) inhibition of rat and human liver glutathione transferases. Taken together, the data suggest that inhibition of glutathione transferase(s) may represent yet another mechanism of retinoid action.
引用
收藏
页码:185 / 189
页数:5
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