Glutathione-mediated conjugation of anticancer drugs: an overview of reaction mechanisms and biological significance for drug detoxification and bioactivation

A Potęga - Molecules, 2022 - mdpi.com
The 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 …

Enterohepatic circulation: physiological, pharmacokinetic and clinical implications

MS Roberts, BM Magnusson, FJ Burczynski… - Clinical …, 2002 - Springer
Enterohepatic recycling occurs by biliary excretion and intestinal reabsorption of a solute,
sometimes with hepatic conjugation and intestinal deconjugation. Cycling is often …

Drug export activity of the human canalicular multispecific organic anion transporter in polarized kidney MDCK cells expressing cMOAT (MRP2) cDNA.

R Evers, M Kool, L van Deemter… - The Journal of …, 1998 - Am Soc Clin Investig
The canalicular (apical) membrane of the hepatocyte contains an ATP-dependent transport
system for organic anions, known as the multispecific organic anion transporter (cMOAT) …

Glutathione and related enzymes in multidrug resistance

ML O'brien, KD Tew - European journal of cancer, 1996 - Elsevier
THE DEVELOPMENT of resistance to chemotherapeutic agents, at concentrations which
were once effective for treatment, is a major obstacle in the clinical treatment of cancers …

Clarifying busulfan metabolism and drug interactions to support new therapeutic drug monitoring strategies: a comprehensive review

AL Myers, JD Kawedia, RE Champlin… - Expert opinion on …, 2017 - Taylor & Francis
ABSTRACT Introduction: Busulfan (Bu) is an alkylating agent with a limited therapeutic
margin and exhibits inter-patient variability in pharmacokinetics (PK). Despite decades of …

Direct observation of negative cooperativity in a detoxification enzyme at the atomic level by Electron Paramagnetic Resonance spectroscopy and simulation

X Bogetti, A Bogetti, J Casto, G Rule, L Chong… - Protein …, 2023 - Wiley Online Library
The catalytic activity of human glutathione S‐transferase A1‐1 (hGSTA1‐1), a homodimeric
detoxification enzyme, is dependent on the conformational dynamics of a key C‐terminal …

Inhibitors of glutathione S-transferases as therapeutic agents

M Schultz, S Dutta, KD Tew - Advanced drug delivery reviews, 1997 - Elsevier
Glutathione S-transferases (GST) are a family of phase II detoxification enzymes with broad
substrate specificities. They catalyze the conjugation of glutathione with many different types …

Anticancer multidrug resistance mediated by MRP1: recent advances in the discovery of reversal agents

A Boumendjel, H Baubichon‐Cortay… - Medicinal research …, 2005 - Wiley Online Library
Abstract Multidrug resistance protein 1 (MRP1) belongs to the ATP‐binding cassette (ABC)
transporter family. It is able to transport a broad range of anticancer drugs through cellular …

Glutathione-related mechanisms in cellular resistance to anticancer drugs.

K Zhang, P Mack, KP Wong - … journal of oncology, 1998 - spandidos-publications.com
Glutathione conjugation and transport of glutathione conjugates of anticancer drugs out of
cells have been shown to work as a system in the detoxification of many anticancer drugs …

Interactions of glutathione S-transferase-π with ethacrynic acid and its glutathione conjugate

S Awasthi, SK Srivastava, F Ahmad, H Ahmad… - … et Biophysica Acta (BBA …, 1993 - Elsevier
Ethacrynic acid, a diuretic drug known to be an inhibitor of glutathione S-transferases
(GSTs), has been shown to enhance the cytotoxicity of the alkylating agent class of …