In recent years, macrocyclic peptides are attracting a growing attention of pharmaceutical/biotech companies and academic groups. Their intermediate size, in-between small-molecule drugs and biotherapeutics, enable their utility as modulators of therapeutically relevant protein-protein interactions (PPIs), while they are still synthetically accessible facilitating medicinal chemistry programs. In this respect, macrocyclic peptides are important chemical tools on the road to PPI modulation to interrogate biological systems and to advance in the treatment of unmet medical needs.
Within the many different types of macrocyclic peptides, the recent focus of attention is on imine-based derivatives. Prominent academic groups are exploiting the imine moiety as a unique source of molecular diversification of macrocyclic peptides, as highlighted in this short compendium.
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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.