Ultra-Short Peptides as Potential Drug Target Molecules in Pharmaceuticals

Dear Colleagues,

Ultra-short peptides (less than seven amino acids) have aroused considerable interest due to their multidisciplinary properties and display great potential in innovative therapies. Due to their small molecular weight, they explore a similar chemical space, combining the advantages of both small organic molecules and therapeutic proteins. They present structural simplicity, which makes their synthesis economically efficient with usually less immunogenicity and cytotoxicity in comparison with longer peptides. Additionally, they exhibit easier tunability and biodegradability, increasing their ability to cross the blood–brain barrier without strictly following Lipinski’s rules. Some of these ultra-short peptides spontaneously self-assemble in water-forming hydrogels due to β-sheet structures, which represent useful sources combining therapeutic and mechanical properties for 3D scaffolds, 3D bioprinting materials, or nanocarriers. Moreover, ultra-short peptides used in the cosmetic industry have not been investigated in depth for other activities in the skin–brain axis; still an unexplored field. Multiple modification options with non-proteogenic amino acids provide a new area between the small organic molecules and the longer peptides.

This Special Issue invites both reviews and original articles that concern the use of ultra-short peptides in the discovery and development of pharmaceuticals. The scope of this Special Issue will cover, but is not limited to, the following: novel synthetic methods in the synthesis of ultra-short peptides, including green chemistry approaches or natural process isolation, medicinal chemistry, structure–activity studies of modified analogs, natural product discovery, drug repositioning, or repurposing of existing short peptides beyond and far pharmaceutical applications.

Dr. Yiannis Sarigiannis
Dr. Christos Petrou
Dr. Evroula Hapeshi
Guest Editors

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