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

被引：13

作者：

Baldassarre, Leonardo ^{[1
]}

Fornasari, Erika ^{[1
]}

Cornacchia, Catia ^{[1
]}

Cirioni, Oscar ^{[2
]}

Silvestri, Carmela ^{[2
]}

Castelli, Pamela ^{[2
]}

Giocometti, Andrea ^{[2
]}

Cacciatore, Ivana ^{[1
]}

机构：

[1] Univ G dAnnunzio, Dept Pharm, Chieti, CH, Italy

[2] Univ Politecn Marche, Osped Riuniti, Clin Infect Dis, Ancona, Italy

来源：

MEDCHEMCOMM | 2013年 / 4卷 / 07期

关键词：

INHIBITOR; DAPTOMYCIN; EFFICACY; ANALOGS; MODEL;

D O I：

10.1039/c3md00122a

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

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.

引用

页码：1114 / 1117

页数：4

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