Genetic selection of cyclic peptide dam methyltransferase inhibitors
Genetic selection of cyclic peptide dam methyltransferase inhibitors
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.
transposition, escherichia-coli, dna methylation, dna adenine methylation, cyclic peptides, peptides, ecodam genetic selection
194-197
Naumann, Todd A.
3046e760-bc90-48a5-bad1-9e3bb2b3112f
Tavassoli, Ali
d561cf8f-2669-46b5-b6e1-2016c85d63b2
Benkovic, Stephen J.
f85498a5-27fc-4a22-9069-ff61a4297520
25 January 2008
Naumann, Todd A.
3046e760-bc90-48a5-bad1-9e3bb2b3112f
Tavassoli, Ali
d561cf8f-2669-46b5-b6e1-2016c85d63b2
Benkovic, Stephen J.
f85498a5-27fc-4a22-9069-ff61a4297520
Naumann, Todd A., Tavassoli, Ali and Benkovic, Stephen J.
(2008)
Genetic selection of cyclic peptide dam methyltransferase inhibitors.
ChemBioChem, 9 (2), .
(doi:10.1002/cbic.200700561).
Abstract
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.
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e-pub ahead of print date: 17 December 2007
Published date: 25 January 2008
Keywords:
transposition, escherichia-coli, dna methylation, dna adenine methylation, cyclic peptides, peptides, ecodam genetic selection
Identifiers
Local EPrints ID: 54487
URI: http://eprints.soton.ac.uk/id/eprint/54487
ISSN: 1439-4227
PURE UUID: bd1b5c27-29df-4f88-8244-3afbcc7f0199
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Date deposited: 19 Aug 2008
Last modified: 16 Mar 2024 03:51
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Author:
Todd A. Naumann
Author:
Stephen J. Benkovic
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