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Genetic selection of cyclic peptide dam methyltransferase inhibitors

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
1439-4227
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
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), 194-197. (doi:10.1002/cbic.200700561).

Record type: Article

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
ORCID for Ali Tavassoli: ORCID iD orcid.org/0000-0002-7420-5063

Catalogue record

Date deposited: 19 Aug 2008
Last modified: 16 Mar 2024 03:51

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Contributors

Author: Todd A. Naumann
Author: Ali Tavassoli ORCID iD
Author: Stephen J. Benkovic

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