Cyclic Peptides in Biological/Medicinal Chemistry

Rosario González-MuñizIn biological and medicinal chemistry, cyclic peptides have advantages over linear analogues, because of their enhanced metabolic stability and a better definition of their conformational mobility. In recent years, there has been a considerable increase in the use of cyclic peptides as tools to better understand relevant biological processes and to search for new therapeutic agents. This was especially important for the study and development of new molecular entities to modulate protein-protein interactions, in which the interfaces are normally large and therefore difficult to target by small-molecules. In this brief note I comment on a few recent representative examples of cyclic peptides useful in biological/medicinal chemistry. In the paper by Low et al. (J. Med. Chem. 2016, 59, 5403), apart of obtaining calpain inhibitors with alternative mode of action, I would like to call the attention on an efficient cyclization method based on a multicomponent reaction, and the need for new, efficient methodologies affording cyclic peptides. The work from Harjani et al. (J. Med. Chem. 2016, 59, 5799) is aimed at finding novel antiinfective agents by targeting underexplored protein-protein interactions, a field of great importance since antibiotic resitance is a real medical burden nowadays. Finally, the publication of Jagtap et al. (J. Med. Chem. 2016, 59, 10190) constitutes a first proof of concet regarding modulation of pre-mRNA splicing, which probably will expand the interest in this process and in the potential of its modulation. It is expected that synthetic advances in cyclization methods and in the conformational control of this type of compounds, along with other applications, such as drug delivery systems, will advance the field of cyclic peptides in the near future.

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Contributed by Rosario González-Muñiz

Rosario is a Senior Researcher at the Medicinal Chemistry Institute (IQM-CSIC), Madrid. She is involved in peptides, secondary structure mimics and small-molecule peptidomimetics of application in biological/medicinal chemistry programs, especially related to the modulation of ion channels and associated proteins.

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