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Mediators of Inflammation
Volume 2012 (2012), Article ID 318087, 22 pages
Review Article

Arginine-Based Inhibitors of Nitric Oxide Synthase: Therapeutic Potential and Challenges

1International Clinical Research Center-Center of Biomolecular and Cell Engineering, St. Anne's University Hospital Brno, 656 91 Brno, Czech Republic
2Institute of Biophysics, Academy of Sciences of the Czech Republic, 612 65 Brno, Czech Republic
3Department of Evolutionary Biology, University of Ferrara, 44100 Ferrara, Italy
4Department of Food and Nutrition, Kyung Hee University, Seoul 130-701, Republic of Korea

Received 2 April 2012; Accepted 30 May 2012

Academic Editor: Hidde Bult

Copyright © 2012 Jan Víteček et al. This is an open access article distributed under the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.


In the past three decades, nitric oxide has been well established as an important bioactive molecule implicated in regulation of cardiovascular, nervous, and immune systems. Therefore, it is not surprising that much effort has been made to find specific inhibitors of nitric oxide synthases (NOS), the enzymes responsible for production of nitric oxide. Among the many NOS inhibitors developed to date, inhibitors based on derivatives and analogues of arginine are of special interest, as this category includes a relatively high number of compounds with good potential for experimental as well as clinical application. Though this group of inhibitors covers early nonspecific compounds, modern drug design strategies such as biochemical screening and computer-aided drug design have provided NOS-isoform-specific inhibitors. With an emphasis on major advances in this field, a comprehensive list of inhibitors based on their structural characteristics is discussed in this paper. We provide a summary of their biochemical properties as well as their observed effects both in vitro and in vivo. Furthermore, we focus in particular on their pharmacology and use in recent clinical studies. The potential of newly designed specific NOS inhibitors developed by means of modern drug development strategies is highlighted.