AI Article Synopsis
- Mycobacterium tuberculosis ribonucleotide reductase (RNR) is identified as a promising target for developing new drugs to combat tuberculosis.
- Researchers focused on creating peptide inhibitors derived from a specific part of the RNR, employing techniques like N-terminal truncation, alanine scanning, and a unique statistical molecular design.
- The study found that certain amino acids (Trp5 and Phe7) are crucial for the effectiveness of these inhibitors, and a quantitative structure-activity relationship model suggested that specific negative charges enhance potency, while a larger side chain could be beneficial at position 5.
Article 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.
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