Triapine
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Triapine
3-Aminopyridine-2-carboxaldehyde thiosemicarbazone (3-AP, also called Triapine) is a substance that is being studied in the treatment of cancer. It belongs to the family of drugs called ribonucleotide reductase inhibitors. 3AP is a potent inhibitor of ribonucleotide reductase, the rate determining enzyme in the supply of deoxynucleotides (DNA building blocks) for DNA synthesis. DNA synthesis is required for cellular proliferation and DNA repair. It is a very strong iron chelator and in the body it is likely that the iron chelate is the active species that quenches the active site tyrosyl radical required by ribonucleotide reductase for its enzymatic activity. The 3AP iron chelate is redox active and there have been several reports in the literature ascribing this property to some of the biological activities of 3AP. 3AP was chosen, based on the results of studying and the screening these products, as the candidate inhibitor most likely to express activity in the setting of human ...
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Ribonucleotide Reductase Inhibitor
Ribonucleotide reductase inhibitors are a family of anti-cancer drugs that interfere with the growth of tumor cells by blocking the formation of deoxyribonucleotides (building blocks of DNA). Examples include: * motexafin gadolinium. * hydroxyurea * fludarabine, cladribine, gemcitabine, tezacitabine, and triapine * gallium maltolate, gallium nitrate See also * Ribonucleotide reductase Ribonucleotide reductase (RNR), also known as ribonucleoside diphosphate reductase (rNDP), is an enzyme that catalyzes the formation of deoxyribonucleotides from ribonucleotides. It catalyzes this formation by removing the 2'-hydroxyl group of th ... References External links Ribonucleotide reductase inhibitorentry in the public domain NCI Dictionary of Cancer Terms Antineoplastic drugs Oxidoreductase inhibitors {{Antineoplastic-drug-stub ...
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