Abstract
A multitude of membrane active peptides exists that divides into subclasses, such as cell penetrating peptides (CPPs) capable to enter eukaryotic cells or antimicrobial peptides (AMPs) able to interact with prokaryotic cell envelops. Peptide membrane interactions arise from unique sequence motifs of the peptides that account for particular physicochemical properties. Membrane active peptides are mainly cationic, often primary or secondary amphipathic, and they interact with membranes depending on the composition of the bilayer lipids. Sequences of these peptides consist of short 5–30 amino acid sections derived from natural proteins or synthetic sources. Membrane active peptides can be designed using computational methods or can be identified in screenings of combinatorial libraries. This review focuses on strategies that were successfully applied to the design and optimization of membrane active peptides with respect to the fact that diverse features of successful peptide candidates are prerequisites for biomedical application. Not only membrane activity but also degradation stability in biological environments, propensity to induce resistances, and advantageous toxicological properties are crucial parameters that have to be considered in attempts to design useful membrane active peptides. Reliable assay systems to access the different biological characteristics of numerous membrane active peptides are essential tools for multi-objective peptide optimization.
Highlights
The smallest self-sustaining biological entities, colloquially called cells, divide into procytes that constitute archaea or bacteria and eucytes that are found in fungi, plants, and animals
A multitude of membrane active peptides exists that divides into subclasses, such as cell penetrating peptides (CPPs) capable to enter eukaryotic cells or antimicrobial peptides (AMPs) able to interact with prokaryotic cell envelops
This review focuses on strategies that were successfully applied to the design and optimization of membrane active peptides with respect to the fact that diverse features of successful peptide candidates are prerequisites for biomedical application
Summary
The smallest self-sustaining biological entities, colloquially called cells, divide into procytes that constitute archaea or bacteria and eucytes that are found in fungi, plants, and animals Cells isolate their interior from the outside world by a protective cover, the core unit of that shield consists of a lipid bilayer called a membrane. In order to utilize these peptides in medical application, it is necessary to optimize their membrane activity and to overcome unwanted effects, such as toxicity or proteolytic degradability [9] According to their mode of interaction, membrane active peptides can be divided into subclasses, such as CPPs that act as membrane transporters while maintaining membrane integrity and AMPs that act as membrane disruptors. Discrimination of the classes of CPPs and AMPs is founded on a historical basis rather than on defined functional differences of peptides attributed to one of the above classes [11]
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