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Design, synthesis and evaluation of peptide inhibitors of Mycobacterium tuberculosis ribonucleotide reductase

✍ Scribed by Johanna Nurbo; Annette K. Roos; Daniel Muthas; Erik Wahlström; Daniel J. Ericsson; Torbjörn Lundstedt; Torsten Unge; Anders Karlén

Book ID
105360724
Publisher
John Wiley and Sons
Year
2007
Tongue
English
Weight
317 KB
Volume
13
Category
Article
ISSN
1075-2617

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✦ Synopsis

Abstract

Mycobacterium tuberculosis ribonucleotide reductase (RNR) is a potential target for new antitubercular drugs. Herein we describe the synthesis and evaluation of peptide inhibitors of RNR derived from the C‐terminus of the small subunit of M. tuberculosis RNR. An N‐terminal truncation, an alanine scan and a novel statistical molecular design (SMD) approach based on the heptapeptide Ac‐Glu‐Asp‐Asp‐Asp‐Trp‐Asp‐Phe‐OH were applied in this study. The alanine scan showed that Trp5 and Phe7 were important for inhibitory potency. A quantitative structure relationship (QSAR) model was developed based on the synthesized peptides which showed that a negative charge in positions 2, 3, and 6 is beneficial for inhibitory potency. Finally, in position 5 the model coefficients indicate that there is room for a larger side chain, as compared to Trp5. Copyright © 2007 European Peptide Society and John Wiley & Sons, Ltd.

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