Recent Trends in Cyclic Peptides as Therapeutic Agents

Dear Colleagues,

For decades, peptides have been utilized as therapeutic agents. There are currently approximately 80 peptide-based drugs on the global market with over 150 peptides in clinical development. Peptides as therapeutics offer several benefits over traditional small molecules, including high specificity, good efficacy, and good safety profiles. These features are tempered by generally lower membrane permeability, shorter half-life, and lower metabolic stability compared to small molecules. However, the use of a cyclic peptide scaffold provides a proven pathway for overcoming these limitations. In recent years, the application of cyclic peptides as therapeutics and novel probes has continued to advance.

There have been several advances in recent years that have continued to broaden the application of cyclic peptides. For example, the development of combinatorial synthesis techniques as well as display (e.g., phage, DNA, mRNA) libraries has exponentially increased the number and breadth of cyclic peptides available to screen in early drug discovery campaigns. The use of novel cyclization strategies (i.e., stapling) as well as non-canonical amino acids further extends the ability to optimize cyclic peptides for clinical and non-clinical applications. In the past decade, cyclic peptides have been approved for a wide range of uses and indications such as antibiotics, obesity, hypoactive sexual desire disorder, irritable bowel syndrome, and lupus nephritis. Cyclic peptides have also shown promise in a number of preclinical studies, including protein–protein interaction inhibitors. They have also been utilized for cell imaging and as drug conjugates, highlighting their potential broad utility.

In this Special Issue, authors are invited to submit original research and review articles highlighting recent trends in cyclic peptides as novel tools and potential therapeutic agents. 

Dr. Marc A. Giulianotti
Prof. Dr. Jutta Eichler
Guest Editors

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