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Genetic Selection of Cyclic Peptide Dam Methyltransferase Inhibitors
Author(s) -
Naumann Todd A.,
Tavassoli Ali,
Benkovic Stephen J.
Publication year - 2008
Publication title -
chembiochem
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.05
H-Index - 126
eISSN - 1439-7633
pISSN - 1439-4227
DOI - 10.1002/cbic.200700561
Subject(s) - peptide , cyclic peptide , selection (genetic algorithm) , in vivo , methyltransferase , chemistry , in vitro , computational biology , biochemistry , biology , computer science , gene , genetics , artificial intelligence , methylation
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 IC 50 of the most active cyclic peptide (SGWYVRNM, shown in the figure) was comparable to that of the known methyltransferase inhibitor, sinefungin.