Peptide molecules are known to play a vital role in important physiological mechanisms, controlling many essential functions in humans such as metabolism, respiration, reproduction, and immune defense. They possess many advantages over other classes of molecule, being small in size, easy to synthesize, and having the ability to penetrate cell membranes. Peptides also have high activity, specificity and affinity, good efficacy and tolerability, as well as biological and chemical diversity. As a result, an increasing number of peptides are entering clinical trials and being approved as drugs. Unfortunately, peptides also carry some significant drawbacks, including limited stability toward proteolysis, poor absorption and transport properties, and interaction with multiple targets (often antibodies), thus inducing antigenicity and unwanted immune response.

The need to address these limitations, and to convert peptides into molecules suitable for medicinal chemistry in drug discovery, has led to the development of peptidomimetics as compounds able to mimic natural peptides and retain the ability to interact with biological targets--thereby producing the same biological effect. Peptidomimetics can be obtained by opportunely controlling the conformational flexibility of the related peptide and/or introducing functional modifications by various synthetic strategies aimed at conferring higher metabolic stability, good bioavailability, and enhanced receptor affinity and selectivity.

In this Research Topic, we wish to highlight recent advances in the development of peptidomimetics. Topics to be addressed include, but are not limited to:

• Design and synthesis of novel peptidomimetics
• Structure-activity relationship studies
• Synthetic strategies for local modifications, secondary structure mimetics and global restrictions
• Structural and physical-chemical characterization
• Pharmacokinetic optimization of novel peptidomimetics
• Applications of peptidomimetics in drug discovery

Submissions addressing the development of peptidomimetics with innovative compositions or synthetic strategy and mechanisms of action are also strongly encouraged. Manuscripts reporting original research and perspectives, as well as reviews and mini-reviews, are welcome.

Prof. Cobb is the founder and director of PepMoTec Limited, a peptide technology spinout company, and has patents in the field. All the other Topic Editors declare no competing interests.

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