Gramicidin
S (GS), one of the oldest commercially used peptide
antibiotics, is known for its robust antibacterial activity against
both Gram-positive and Gram-negative bacterial strains. Although it
was discovered well over 70 years ago, its clinical potential was
limited to topical applications because of its high hemolytic activity.
To overcome this side effect, significant efforts have been invested
in the chase for GS analogues with high therapeutic index (e.g., high
antimicrobial activity and low hemolytic activity) in the past decades.
In this Perspective, the structural properties and biological profiles
(including the recently discovered activities) of representative GS
analogues designed by different approaches are described and analyzed.
We also present how the general structure–activity relationships
were established and how they could help in the design of more efficient
GS analogues.
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