Involvement of human glutathione S-transferase M1-1 in the glutathione conjugation of the antitumor unsymmetrical bisacridine derivative C-2028. - Open Research Data - Bridge of Knowledge

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Involvement of human glutathione S-transferase M1-1 in the glutathione conjugation of the antitumor unsymmetrical bisacridine derivative C-2028.

Description

Unsymmetrical bisacridines (UAs) are a novel potent class of antitumor-active therapeutics. The aim of this study was to investigate the possible role of human glutathione S-transferase M1-1 (hGSTM1-1) in the glutathione (GSH) conjugation of a representative UA, C‑2028.

0.05 mg/mL recombinant hGSTM1-1 (expressed in Escherichia coli, obtained from Sigma-Aldrich, MO, USA), 0.01 mM C-2028, and 5 mM reduced L-glutathione (GSH) in 0.1 M Hepes buffer solution (pH 6.5) were incubated at 37 °C for 0 and 1 hrs in a total volume of 50 µL. MgCl2 solution (2 mM) was added for enzyme stimulation. The incubations were terminated by adding ice-cold 1 M HCl to the incubation mixtures (10:90, v/v). The samples were vortexed, placed in ice for 10 min, and centrifuged at 10000 x g for 10 min. Aliquots of the supernatants (50 µL) in triplicate were then analyzed directly by reversed-phase liquid chromatography (RP-LC) with UV-vis detection and/or diode array and multiple wavelength detection, and monitored by MS.

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License:
Creative Commons: by-nc-sa 4.0 open in new tab
CC BY-NC-SA
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Details

Year of publication:
2021
Verification date:
2021-06-10
Dataset language:
English
Fields of science:
  • chemical sciences (Natural sciences)
DOI:
DOI ID 10.34808/p6dd-5469 open in new tab
Verified by:
Gdańsk University of Technology

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