Wyszukiwarka
Filtry
wszystkich: 8
Wyniki wyszukiwania dla: enzymatic conjugation
-
Novel insights into conjugation of antitumor-active unsymmetrical bisacridine C-2028 with glutathione: characteristics of non-enzymatic and glutathione S-transferase-mediated reactions
PublikacjaUnsymmetrical bisacridines (UAs) are a novel potent class of antitumor-active therapeutics. A significant route of phase II drug metabolism is conjugation with glutathione (GSH), which can be non-enzymatic and/or catalyzed by GSH-dependent enzymes. The aim of this work was to investigate the GSH-mediated metabolic pathway of a representative UA, C 2028. GSH supplemented incubations of C-2028 with rat, but not with human, liver...
-
Non-enzymatic glutathione-mediated conjugation of unsymmetrical bisacridine C-2028 with anticancer activity
Dane BadawczeThe presented data complement the studies on the interplay between C-2028 (anticancer-active unsymmetrical bisacridine) and the glutathione S-transferase/glutathione (GST/GSH) system.
-
Glutathione-mediated conjugation of anticancer drugs: an overview of reaction mechanisms and biological significance for drug detoxification and bioactivation.
PublikacjaThe effectiveness of many anticancer drugs depends on the creation of specific metabolites that may alter their therapeutic or toxic properties. One significant route of biotransformation is a conjugation of electrophilic compounds with reduced glutathione, which can be non-enzymatic and/or catalyzed by glutathione-dependent enzymes. Glutathione usually combines with anticancer drugs and/or their metabolites to form more polar...
-
Enzyme Conjugation - A Promising Tool for Bio-catalytic and Biotransformation Applications – A Review
PublikacjaEnzymes have revolutionized conventional industrial catalysts as more efficient, eco-friendly, and sustainable substitutes that can be used in different biotechnological processes, food, and pharmaceutical industries. Yet, the enzymes from nature are engineered to make them adapt and enhance their durability in the industrial environment. One promising approach involves the combined use of multiple enzymes that catalyze highly...
-
New Chalcones Derivatives With Potent Antitumor Activity And Their Metabolism In Vitro
PublikacjaChalcone derivatives exhibit a broad range of biological activities, with antioxidant and cytotoxic properties among the most studied. Despite numerous reports on chalcones as cytotoxic, and potentially anticancer agents, very little is know on their actual mechanism of activity. Generally, chalcones are considered as antimitotic agents, which interfere with tubulin assembly.We have recently developed a new class of chalcones with...
-
Phase I and phase II metabolism simulation of antitumor-active 2-hydroxyacridinone with electrochemistry coupled on-line with mass spectrometry.
PublikacjaHere, we report the metabolic profile and the results of associated metabolic studies of 2-hydroxyacridinone (2-OH-AC), the reference compound for antitumor-active imidazo- and triazoloacridinones. Electrochemistry coupled with mass spectrometry was applied to simulate the general oxidative metabolism of 2-OH-AC for the first time. The reactivity of 2-OH-AC products to biomolecules was also examined. The usefulness of the electrochemistry...
-
Glutathione conjugation of the antitumor-active 1-nitroacridine derivatives compounds C-857 and C-1748 – the major role of glutathione S-transferase M1-1
Dane BadawczeObjectives: C-857 and C-1748 are antitumor-active agents, monomers of unsymmetrical bisacridine derivatives. The aim of this study was to analyze their glutathione (GSH) conjugation in vitro in the presence of glutathione S-transferase (GST) M1-1.
-
Involvement of human glutathione S-transferase M1-1 in the glutathione conjugation of the antitumor unsymmetrical bisacridine derivative C-2028.
Dane BadawczeUnsymmetrical 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.