Genetic Selection of Cyclic Peptide Dam Methyltransferase Inhibitors

Abstract

Let's go round. We report the development of a transposition based genetic selection methodology used to uncover three cyclic peptide inhibitors of the E. coli methyltransferase. The activity of the selected cyclic peptides was confirmed in vivo and in vitro. The IC50 of the most active cyclic peptide (SGWYVRNM, shown in the figure) was comparable to that of the known methyltransferase inhibitor, sinefungin. Supporting information for this article is available on the WWW under http://www.wiley-vch.de/contents/jc_2268/2008/z700561_s.pdf or from the author. Please note: The publisher is not responsible for the content or functionality of any supporting information supplied by the authors. Any queries (other than missing content) should be directed to the corresponding author for the article.