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Antimicrobial peptides (AMPs) are found virtually in every living organism providing an immediate defence against pathogen invasion and constitute a challenging opportunity to be developed as therapeutical molecules. Many efforts are actually devoted to bring AMPs into clinical use especially because of the rapidly worldwide resistance development to conventional antibiotics. With no attempt to present a comprehensive overview of all AMPs being assessed as potential pharmacological agents, in this chapter we provide an overview of the biological role, classification, and mode of action of AMPs; besides antimicrobial activity, we also briefly describe the modulation of the immune response, the enhancement of angiogenesis and wound healing, and the prevention of post-surgical adhesions. We tackle the challenges of developing AMPs for clinical applications, and present an overview of innovative formulation/delivery strategies. In particular, we illustrate the relationships between their biophysical features and activities. The current status and future directions in the development of AMP therapeutics with efforts spanning a multitude of disciplines from chemistry, physics, biology to materials and contributing to the development of highly active AMPs are also discussed.

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