Stephan Köhler and Jean-Yves Winum from CNRS, and their colleagues, have created a new series of inhibitors that are highly active in vitro, and are shown to be active in vivo. Additionally, molecular modelling and competition experiment with NAD+ confirmed the positioning of the inhibitor inside the active site of HDH. As the target HDH has been directly linked to bacterial virulence, and with the results obtained on live extra- and intracellular brucellae, the development of these inhibitors can be considered as a promising step towards novel anti-virulence drugs.
The referees thought this article was very significant, and so do we – so read this HOT article today in OBC. It is free to download until 5th May.
Anti-virulence Strategy against Brucella suis: Synthesis, Biological Evaluation and Molecular Modeling of Selective Histidinol Dehydrogenase Inhibitors
Marie-Rose Abdo, Pascale Joseph, Jérémie Mortier, François Turtaut, Jean-Louis Montero, Bernard Masereel, Stephan Köhler and Jean-Yves Winum
Org. Biomol. Chem., 2011, Advance Article