| Literature DB >> 18061679 |
Jill M Kolesar1, William R Schelman, Peter G Geiger, Kyle D Holen, Anne M Traynor, Dona B Alberti, James P Thomas, Christopher R Chitambar, George Wilding, William E Antholine.
Abstract
The metal chelator Triapine, 3-aminopyridine-2-carboxaldehyde thiosemicarbazone, is a potent inhibitor of ribonucleotide reductase. EPR spectra consistent with signals from Fe-transferrin, heme, and low-spin iron or cupric ion were observed in peripheral blood mononuclear cells (PBMCs) obtained from patients treated with Triapine. One signal that is unequivocally identified is the signal for Fe-transferrin. It is hypothesized that Fe uptake is blocked by reactive oxygen species generated by FeT(2) or CuT that damage transferrin or transferrin receptor. A potential source for the increase in the heme signal is cytochrome c released from the mitochondria. These results provide valuable insight into the in vivo mechanism of action of Triapine.Entities:
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Year: 2007 PMID: 18061679 PMCID: PMC2390869 DOI: 10.1016/j.jinorgbio.2007.10.013
Source DB: PubMed Journal: J Inorg Biochem ISSN: 0162-0134 Impact factor: 4.155