Factors Affecting Nitroreductase Activity in the Biological Reduction of Nitro Compounds

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Abstract:

Nitro compounds are used in various industries, including the pharmaceutical industry. These compounds have considerable importance for human health for two distinctly different reasons. Some nitro compounds are toxic environmental contaminants and pose a serious threat to human health; others are used as therapeutic agents. Nitro compounds are used as agents for the treatment of infectious diseases caused by Grampositive and Gram-negative bacteria, as antifungal and antiparasitic drugs, and as chemotherapeutic agents. To exert either beneficial or adverse biological effects, nitro compounds require enzymatic activation, either by nitroreduction alone or by ring oxidation followed by nitroreduction. The mechanism of drug action relies on the toxicity of the products generated by nitroreductases. Nitroreductases differ in the range of specificity and levels of activity with various nitro prodrugs. In this review, factors affecting nitroreductase activity, especially compounds that inhibit reduction, will be discussed.

Keywords: antimicrobial; environment; mutagen; nitro compounds; nitroreductases; pharmaceutical; prodrugs; therapeutics

Document Type: Review Article

DOI: http://dx.doi.org/10.2174/157340805774580420

Affiliations: Division of Microbiology, National Center for Toxicological Research, U.S. FDA, Jefferson, AR 72079, USA.

Publication date: November 1, 2005

More about this publication?
  • Current Enzyme Inhibition aims to publish all the latest and outstanding developments in enzyme inhibition studies with regards to the mechanisms of inhibitory processes of enzymes, recognition of active sites, and the discovery of agonists and antagonists, leading to the design and development of new drugs of significant therapeutic value. Each issue contains a series of timely, in-depth reviews written by leaders in the field, covering a range of enzymes that can be exploited for drug development. Current Enzyme Inhibition is an essential journal for every pharmaceutical and medicinal chemist who wishes to have up-to-date knowledge about each and every development in the study of enzyme inhibition.
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