Journal ArticleDOI
Bioactivation of S-methyl N,N-Diethylthiolcarbamate to S-methyl N,N-diethylthiolcarbamate sulfoxide: Implications for the role of cytochrome P450
Bruce W. Hart,Morris D. Faiman +1 more
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DETC-MeSO was found to be a potent inhibitor of rat liver mitochondrial low Km ALDH both in vivo and in vitro, and that inhibition of cytochrome P450 by inhibitors such as NBI block the inhibition of low KM ALDH by DETC-me.About:
This article is published in Biochemical Pharmacology.The article was published on 1993-12-14. It has received 33 citations till now. The article focuses on the topics: Aldehyde dehydrogenase & Cytochrome P450.read more
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Dithiocarbamates Induce Apoptosis in Thymocytes by Raising the Intracellular Level of Redox-active Copper
TL;DR: It is concluded that pyrrolidine dithiocarbamate exerts a powerful pro-oxidant effect on thymocytes due to its ability to transport external redox-active copper into cells.
Journal ArticleDOI
Degradation of the thiocarbamate herbicide EPTC (S-ethyl dipropylcarbamothioate) and biosafening by Rhodococcus sp. strain NI86/21 involve an inducible cytochrome P-450 system and aldehyde dehydrogenase.
TL;DR: It was demonstrated that the aldehyde dehydrogenase gene is widespread in the Rhodococcus genus, but the components of the cytochrome P-450 system are unique to Rhoditis sp.
Journal ArticleDOI
Inhibition of aldehyde dehydrogenase by disulfiram and its metabolite methyl diethylthiocarbamoyl-sulfoxide.
TL;DR: Observations are consistent with mechanisms where inhibition of aldehyde dehydrogenase by DSF in vitro involves oxidation of the active site, whereas MeDTC-SO forms a covalent adduct with the protein in vitro resulting in cessation of enzyme activity.
Journal ArticleDOI
Disulfiram's anti-cancer activity reflects targeting NPL4, not inhibition of aldehyde dehydrogenase.
Zdenek Skrott,Dusana Majera,Jan Gursky,Tereza Buchtova,Marian Hajduch,Martin Mistrik,Jiri Bartek,Jiri Bartek +7 more
TL;DR: It is shown that DSF does not directly inhibit ALDH activity in diverse human cell types, while DSF’s in vivo metabolite, S-methyl-N,N-diethylthiocarbamate-sulfoxide inhibits AL DH activity yet does not impair cancer cell viability, clarifying the confusing literature about the anti-cancer mechanism of DSF.
Journal ArticleDOI
Role of disulfiram in the in vitro inhibition of rat liver mitochondrial aldehyde dehydrogenase
TL;DR: It is reported here that when disulfiram inhibited recombinant rat liver mitochondrial ALDH in vitro, no significant molecular mass increase was detected during the first 30 min as determined by on-line HPLC-electrospray ionization mass spectrometry (LC-MS), which indicated that the inhibition in vitro was not caused directly by covalent adduct formation on the enzyme.
References
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Journal ArticleDOI
The subcellular distribution and properties of aldehyde dehydrogenases in rat liver.
TL;DR: Kinetic experiments suggested the possible existence of at least two different NAD(+)-dependent aldehyde dehydrogenases in rat liver and distribution studies showed that one enzyme, designated enzyme I, was exclusively localized in the mitochondria and that another enzyme, designate enzyme II, was localized in both the mitochondia and the microsomal fraction.
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Metabolism of disulfiram and diethyldithiocarbamate in rats with demonstration of an in vivo ethanol-induced inhibition of the glucuronic acid conjugation of the thiol.
TL;DR: Evidence was obtained indicating that ethanol lowers the rate by which diethyldithiocarbamate is conjugated with glucuronic acid, which is related to the ethanol sensitizing effect of disulfiram.
Journal ArticleDOI
Substituted imidazoles as inhibitors of microsomal oxidation and insecticide synergists
TL;DR: Several of the 1-arylimidazoles are potent in vivo synergists of carbaryl against NAIDM insecticide susceptible houseflies and bind powerfully to cytochrome P-450 and yield type II difference spectra in oxidized and NADPH-reduced microsomes.
Journal Article
The rapid reduction of disulfiram in blood and plasma.
TL;DR: A gas chromatographic assay procedure was developed to quantitate the reduction product of disulfiram, diethyldithiocarbamate (DDC), in blood and plasma and found that the DDC formed decomposed in human and dog blood with half-lives of 70 and 100 minutes, respectively.
Related Papers (5)
In vitro and in vivo inhibition of rat liver aldehyde dehydrogenase by s-methyl N, N-diethylthiolcarbamate sulfoxide, a new metabolite of disulfiram
Bruce W. Hart,Morris D. Faiman +1 more