Dear Colleagues,

Bioactive peptides are formed by amino acids (50 or less), which can perform hormonal and signaling functions in the human body. Although they were first only used as a model for the development of small molecules, peptides are now considered important drug candidates and peptide-based drug discovery has had a renaissance. Peptides fill the gap between small molecules and protein-based therapeutics in terms of molecular dimensions and display some virtues, including elevated target selectivity, reduced side effects and toxic degradation products. More than 100 FDA-approved peptide-based medicines are already available on the pharmaceutical market, and a robust clinical pipeline is currently enrolling numerous peptide molecules. For instance, therapeutic peptides enable alternative treatments for several conditions such as diabetes, cancer, obesity, osteoporosis, cardiovascular diseases, and inflammation. In conjugation with carriers or nanoparticles, the employment of chemical strategies to improve the ‘drug-like’ properties of peptides have helped to address their critical pharmacokinetic issues. Moreover, the advancements in the synthetic technologies that can smoothly provide large peptide libraries, along with reduced costs and a more sustainable approach, are encouraging their use for further biomedical investigations. In this Special Issue, we intend to present the most recent topics and advances, which could be useful in the design and pharmacological investigations of bioactive peptides, looking at challenging pathological conditions. Papers on the identification and characterization of novel peptides, elucidation of their mechanism of action, and strategies employed to improve their ‘drug-like’ properties are welcome.

Dr. Francesco Merlino
Dr. Rosa Bellavita
Guest Editors

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• bioactive peptides
• peptidomimetics
• therapeutic peptides
• drug discovery
• conjugated peptides
• cell penetrating peptides
• protein-protein interactions
• peptide-based delivery
• beta-amino acids