Trends Pharmacol Sci. 2008 Feb 8 [Epub ahead of print] Volume 29, Issue 3, March 2008, Pages 124-134

The bacterial envelope as a target for novel anti-MRSA antibiotics.

Van Bambeke F, Mingeot-Leclercq MP, Struelens MJ, Tulkens PM.

Université Catholique de Louvain, Unité de Pharmacologie Cellulaire et
Moléculaire, UCL 7370 Avenue Mounier 73, 1200 Brussels, Belgium.

Methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-intermediate S.
aureus (VISA) are spreading worldwide, making the search for antibiotics directed
against new targets a high priority. Drugs that anchor in the bacterial membrane 
(e.g. ceragenins and lipopeptides) or that target the bacterial membrane and
proteic (lipoglycopeptides) or lipidic (glycodepsipeptides) cell wall precursors 
seem to have the most potential because they show a fast and extensive
bactericidal effect and are probably less prone to select for resistance owing to
the difficulty in modifying their targets in a way that is compatible with
bacterial survival. The efficacy of lipopeptides and lipoglycopeptides has been
demonstrated in the treatment of skin and skin structure infections, and
bacteremia caused by resistant S. aureus. Ceragenins and glycodepsipeptides are
restricted to topical applications because of their unsatisfactory safety
profile. The mode of action, pharmacological and microbiological properties and
target indications of these anti-MRSA agents, which function by disturbing
membrane integrity, are reviewed in this article.

PMID: 18262289 [PubMed - as supplied by publisher]

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