Masters, JRW and Know, RJ and Hartley, JA and Kelland, LR and Hendriks, HR and Connors, T (1997) KW-2149 (7-N-[2-[Y-L-glutamylamino]ethyldithioethyl]mitomycin C) - A new mitomycin C analogue activated by serum. BIOCHEM PHARMACOL , 53 (3) 279 - 285.
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KW-2149 (7-N-[2-[Y-L-glutamylamino]ethyldithioethyl]mitomycin C) is a new mitomycin-C analogue in clinical trial. This study demonstrates that KW-2149, unlike mitomycin C, is activated to a cytotoxic species by extracellular metabolism in serum. The metabolising activity differs between batches of serum and species of origin. Human serum had high activity (which resulted in a 150-fold enhancement of cytotoxicity), whereas mouse serum had low activity. In the presence of serum, the rate of uptake of H-3-KW-2149 into cells increased by 8-fold and drug binding to DNA by 32-fold. The metabolising activity of serum can partially be replaced by glutathione. No anticancer drug has previously been described whose toxicity is mediated by metabolism in serum. Copyright (C) 1997 Elsevier Science Inc.
|Title:||KW-2149 (7-N-[2-[Y-L-glutamylamino]ethyldithioethyl]mitomycin C) - A new mitomycin C analogue activated by serum|
|Keywords:||new anticancer agent, mitomycin C, intravesical chemotherapy, bladder cancer, serum factor, drug metabolism, ANTITUMOR-ACTIVITY, CELL-LINES, RESISTANT, INVITRO, MURINE|
|UCL classification:||UCL > School of Life and Medical Sciences > Faculty of Medical Sciences > Surgery and Interventional Science (Division of) > Research Department of Urology|
UCL > School of Life and Medical Sciences > Faculty of Medical Sciences > Wolfson Institute and Cancer Institute Administration > Cancer Institute > Research Department of Oncology
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