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Issue 7, 2013
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Discovery of novel RIP derivatives by alanine scanning for the treatment of S. aureus infections

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Abstract

Alanine scanning has been used to define the key residues for the activity of RNA III inhibiting peptide (RIP) against S. aureus. We have found that the threonine residue at position 5 is detrimental to the RIP activity, while the removal of serine (P2) and phenylalanine (P7) afforded the most active RIP derivatives (2 and 7). Moreover, we have identified the small RIP derivative (9), corresponding to the sequence H-Ser-Pro-Trp-Thr-NH2, which displayed the best antistaphylococcal activity.

Graphical abstract: Discovery of novel RIP derivatives by alanine scanning for the treatment of S. aureus infections

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Publication details

The article was received on 23 Apr 2013, accepted on 15 May 2013 and first published on 15 May 2013


Article type: Concise Article
DOI: 10.1039/C3MD00122A
Citation: Med. Chem. Commun., 2013,4, 1114-1117
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    Discovery of novel RIP derivatives by alanine scanning for the treatment of S. aureus infections

    L. Baldassarre, E. Fornasari, C. Cornacchia, O. Cirioni, C. Silvestri, P. Castelli, A. Giocometti and I. Cacciatore, Med. Chem. Commun., 2013, 4, 1114
    DOI: 10.1039/C3MD00122A

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