Issue 7, 2013
From the journal:

MedChemComm

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

Leonardo Baldassarre,a   Erika Fornasari,a   Catia Cornacchia,a   Oscar Cirioni,b   Carmela Silvestri,b   Pamela Castelli,b   Andrea Giocomettib  and  Ivana Cacciatore*a  

* Corresponding authors

a Department of Pharmacy, University of Chieti-Pescara, Via dei Vestini 31, Chieti Scalo (CH), Italy
E-mail: cacciatore@unich.it
Fax: +39 871 3554470
Tel: +39 871 3554475

b Clinic of Infectious Diseases, Università Politecnica delle Marche – Ospedali Riuniti, Ancona, Italy

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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Article information

DOI
https://doi.org/10.1039/C3MD00122A
Article type
Concise Article
Submitted
23 Apr 2013
Accepted
15 May 2013
First published
15 May 2013

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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