An NSAID. Circumvents MRP-mediated multidrug resistance. Significantly increases the cytotoxicity of the anthracyclines (doxorubicin, daunorubicin and epirubicin), as well as teniposide, VP-16 and vincristine.
Chemical research in toxicology, 18(11), 1729-1736 (2005-11-23)
Zomepirac [ZP, 5-(chlorobenzoyl)-1,4-dimethylpyrrole-2-acetic acid] was withdrawn from the market because of unpredictable allergic reactions that may have been caused by ZP-protein adducts formed by reaction of the reactive acyl glucuronide of ZP (ZP-O-G) with endogenous proteins. To test the hypothesis
Social science & medicine (1982), 46(1), 39-51 (1998-02-17)
This article systematically examines government regulation of medicines in the U.K. and the U.S. with specific reference to carcinogenic risk assessment. By taking four non-steroidal anti-inflammatory drugs (NSAIDs) as case studies, it is argued that there have been inconsistencies between
Journal of pharmacological and toxicological methods, 41(1), 27-32 (1999-10-03)
The covalent binding of drugs or their metabolites to proteins is of increasing interest in the investigation of the toxicity of these compounds. Recent attention on biological consequences of protein adduct formation with carboxylate drugs, derived via their reactive acyl
Chemical research in toxicology, 9(3), 659-666 (1996-04-01)
Carboxylate drugs usually form acyl glucuronide conjugates as major metabolites. These electrophilic metabolites are reactive, capable of undergoing hydrolysis, rearrangement, and covalent binding reactions to proteins. The last-mentioned property has the potential to initiate immune and other toxic responses in
Many nonsteroidal anti-inflammatory drugs (NSAIDs) which have antiproliferative activity in colon cancer cells are carboxylate compounds forming acyl glucuronide metabolites. Acyl glucuronides are potentially reactive, able to hydrolyse, rearrange into isomers, and covalently modify proteins under physiological conditions. This study
Protein-based drug transporters are expressed in Sf9 cells. Understanding the specific mechanisms of tumor cell transporters is an essential aspect of chemotherapeutic drug design.
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