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Benzimidazolone activators of chloride secretion: potential therapeutics for cystic fibrosis and chronic obstructive pulmonary disease.
TLDR
Compared with 1-EBIO, the most potent of these derivatives, DCEBIO was severalfold better in a 86Rb+ uptake assay, 20-fold better in short circuit current measurements on T84 monolayers, and 100-foldbetter in patch-clamp assays of hIK1 activity. Expand
Activity of four allelic forms of glutathione S-transferase hGSTP1-1 for diol epoxides of polycyclic aromatic hydrocarbons.
  • X. Hu, H. Xia, +5 authors S. Singh
  • Chemistry, Medicine
  • Biochemical and biophysical research…
  • 18 September 1997
TLDR
It is proposed that amino acid 113 functions as part of a clamp that lines the mouth of the water channel leading to the active sites of the hGSTP1-1 dimer and controls the access to substrates, and the hydrophobicity and the size of residue 113 are important in co-determining the substrate specificity of the isoenzymes. Expand
Differential catalytic efficiency of allelic variants of human glutathione S-transferase Pi in catalyzing the glutathione conjugation of thiotepa.
TLDR
It is reported that the allelic variants of human Pi class GST (hGSTP1-1), which differ in their primary structures at amino acids in positions 104 and/or 113, exhibit significant differences in their activity in the GSH conjugation of alkylating anticancer drug thiotepa. Expand
Hepatic xenobiotic metabolizing enzymes in two species of benthic fish showing different prevalences of contaminant-associated liver neoplasms.
TLDR
Differences in enzyme activities and isoenzyme profiles suggest a toxicological basis which may help to explain the differences in prevalences of contaminant-associated liver neoplasms between these two species. Expand
Accelerated Metabolism and Exclusion of 4-Hydroxynonenal through Induction of RLIP76 and hGST5.8 Is an Early Adaptive Response of Cells to Heat and Oxidative Stress*
TLDR
Stress-pre-conditioned cells with induced hGST5.8 and RLIP76 acquired resistance to 4-HNE and H2O2-mediated apoptosis by suppressing a sustained activation of c-Jun N-terminal kinase and caspase 3, suggesting a role of LPO products, particularly 4- HNE, in the initial phase of stress mediated signaling. Expand
Novel function of human RLIP76: ATP-dependent transport of glutathione conjugates and doxorubicin.
TLDR
Results indicate that RLIP76, in addition to its role in signal transduction, can catalyze transport of glutathione conjugates and xenobiotics, and may contribute to the multidrug resistance phenomenon. Expand
Differential induction of NAD(P)H:quinone oxidoreductase by anti-carcinogenic organosulfides from garlic.
TLDR
The results of the present study suggest that induction of NQO may be important in anti-cancer effects of garlic OSCs. Expand
Adenosine triphosphate-dependent transport of doxorubicin, daunomycin, and vinblastine in human tissues by a mechanism distinct from the P-glycoprotein.
TLDR
It is demonstrated for the first time that a membrane protein that catalyzed the transport of anionic amphiphilic molecules such as glutathione conjugates could also mediate the transportof weakly cationic antitumor antibiotic, doxorubicin. Expand
Two distinct 4-hydroxynonenal metabolizing glutathione S-transferase isozymes are differentially expressed in human tissues.
TLDR
HGST5.8 and hGSTA4-4 are demonstrated to be distinct human glutathione S-transferase isozymes, and there are significant differences in their kinetic properties. Expand
Mechanism of inhibition of benzo[a]pyrene-induced forestomach cancer in mice by dietary curcumin.
TLDR
The results of the present study suggest that curcumin may inhibit BaP-induced forestomach cancer in mice by affecting both activation as well as inactivation pathways of BaP metabolism in the liver. Expand
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