Journal of Synthetic Organic Chemistry, Japan
Online ISSN : 1883-6526
Print ISSN : 0037-9980
ISSN-L : 0037-9980
Constrained Peptides in Drug Discovery and Development
Douglas R. CaryMasaki OhuchiPatrick C. ReidKeiichi Masuya
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2017 Volume 75 Issue 11 Pages 1171-1178


Constrained peptides, namely macrocyclic and stapled peptides, are receiving increasing attention as a promising class of compounds for the inhibition of protein-protein interactions (PPI). The current state of peptide therapeutics is discussed, including their merits and challenges, as well as recent technological developments that have enabled a new era in peptide research and development. The technology behind PeptiDream’s Peptide Discovery Platform System (PDPS) is described, showing how it can be used to rapidly generate libraries of constrained peptides and obtain detailed SAR information. This technology can provide, with a high rate of success, potent peptide ligands that may be developed as drug candidates themselves, utilized in peptide-drug conjugates (PDC), or converted into small molecule drug leads. The outlook for the field of constrained peptides and their use in the clinic is also described.

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© 2017 The Society of Synthetic Organic Chemistry, Japan
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