Ethacrynic acid and its glutathione conjugate as inhibitors of glutathione S-transferases

J Ploemen, B Ommen, JJP Bogaards… - Xenobiotica, 1993 - Taylor & Francis
1. The diuretic drug ethacrynic acid (EA) is a potent reversible inhibitor of rat and human
glutathione S-transferases (GST), with I 50-values (πm) of 4.6–6.0, 0.3–1.9 and 3.3–4.8 π, π …

Inhibition of glutathione S-transferase activity in human melanoma cells by α, β-unsaturated carbonyl derivatives. Effects of acrolein, cinnamaldehyde, citral …

MLPS van Iersel, JPHTM Ploemen, I Struik… - Chemico-biological …, 1996 - Elsevier
The glutathione S-transferase (GST) activity towards 1-chloro-2, 4-dinitrobenzene in intact
human IGR-39 melanoma cells was determined by the quantification by HPLC-analysis of …

Expression of paclitaxel-inactivating CYP3A activity in human colorectal cancer: implications for drug therapy

C Martinez, E Garcia-Martin, RM Pizarro… - British journal of …, 2002 - nature.com
Cytochrome P450 3A is a drug-metabolising enzyme activity due to CYP3A4 and CYP3A5
gene products, that is involved in the inactivation of anticancer drugs. This study analyses …

Design, Synthesis, and Structure−Activity Relationships of Haloenol Lactones:  Site-Directed and Isozyme-Selective Glutathione S-Transferase Inhibitors

Z Wu, GS Minhas, D Wen, H Jiang… - Journal of medicinal …, 2004 - ACS Publications
Overexpression of glutathione S-transferase (GST), particularly the GST-π isozyme, has
been proposed to be one of the biochemical mechanisms responsible for drug resistance in …

Conjugation of glutathione and other thiols with bioreductively activated mitomycin C. Effect of thiols on the reductive activation rate

M Sharma, M Tomasz - Chemical research in toxicology, 1994 - ACS Publications
Mitomycin C (MC), a clinically used natural antitumor agent, was shown toform three
monoconjugates (1la-13a) and two bisconjugates (14a, 15a) with GSH upon reductive …

Enhanced cytotoxicity of bioreductive antitumor agents with dimethyl fumarate in human glioblastoma cells

B Gu, LM DeAngelis - Anti-cancer drugs, 2005 - journals.lww.com
We compared the cytotoxicity of the bioreductive antitumor agents mitomycin C (MMC) and
streptonigrin (SN) with or without the DT-diaphorase (DTD) inducer dimethyl fumarate (DMF) …

The molecular toxicology of mitomycin C

MM Paz, CA Pritsos - Advances in Molecular Toxicology, 2012 - Elsevier
The drug mitomycin C (MMC) is used in the clinic for the chemotherapy of several types of
cancer. Two distinctive features define the mode of action of MMC: First, it is a prodrug that …

Molecular targeting of mitomycin C chemotherapy

M Nishiyama, K Suzuki, T Kumazaki… - … journal of cancer, 1997 - Wiley Online Library
In 10 human cancer cell lines, the activity of mitomycin C (MMC) was found to be determined
by an interplay between activation by DT‐diaphorase (DTD) and inactivation by glutathione …

Non-cross resistance of ZD0473 in acquired cisplatin-resistant lung cancer cell lines

Y Kawamura-Akiyama, H Kusaba, F Kanzawa… - Lung Cancer, 2002 - Elsevier
ZD0473 is a new generation platinum agent that, in preclinical studies, shows evidence of
an extended spectrum of anti-tumor activity and overcomes platinum resistance …

Mechanism of differential sensitivity of human bladder cancer cells to mitomycin C and its analogue

BH Xu, V Gupta, SV Singh - British journal of cancer, 1994 - nature.com
This study was undertaken to elucidate the mechanism (s) of differential sensitivity of human
bladder cancer cell lines J82 and SCaBER to mitomycin C (MMC) and its analogue, BMY …