Cyclic peptides are a unique class of molecules that combine the specificity and
larger interactive surface area of biological molecules with the favorable drug-like properties
of a small molecule, including pharmacokinetic enhancements and proteolytic stability.
There is much interest in the development and characterization of cyclic peptides as potential
drug leads. Additionally, in the field of peptidomimetics, cyclic peptides can prove vital
as probes for understanding cellular processes, such as cell penetration and modulation of
signaling pathways. Cyclic peptides have great potential as therapeutics for a wide variety of diseases, targeting
different mechanisms of cancer, HIV proliferation, inflammation in skin disorders, and cell survival in
neurodegenerative diseases. Novel synthetic strategies for tethering cyclic peptides in a ring, including biosynthetic
methods, create a large range of macrocyclic peptidomimetic compounds, opening the field to further
drug design possibilities as well as novel chemical biological probes. Current studies within each of these
areas in the cyclic peptide arena are described herein.
Keywords: Antibiotics, macrocycle, peptide therapeutics, peptidomimetics, signaling, β-turn
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