Antimicrobial Peptides (AMPs) are short amphipathic biological molecules generally
with less than 100 amino acids. AMPs not only present high bioactivities against bacteria, fungi or
protists-induced infections, but also play important roles in anticancer activity, immune response
and inflammation regulation. AMPs are classified as ribosomally synthesized, non-ribosomally
synthesized and post-translationally modified, non-ribosomally synthesized ones and several
synthetic or semisynthetic peptides according to their synthesis with or without the involvement of
ribosomes. The molecular characterization and bioactivity action mechanisms are summarized for
several ribosomally synthesized AMPs and main non-ribosomally synthesized members
(cyclopeptides, lipopeptides, glycopeptides, lipoglycopeptides). We also analyze challenges and
new strategies to overcome drug resistance and application limitations for AMP discovery. In
conclusion, the growing novel small molecular AMPs have huge therapeutic potentials of
antibacterial, antiviral, anticancer and immunoregulatory bioactivities through new techniquesdriven
drug discovery strategy including bioinformatics prediction, de novo rational design and
biosynthesis.
Molecular Action Mechanisms and Membrane Recognition of Membrane-Acting Antimicrobial Peptides