著者

Douglas R. Cary 大内 政輝 Patrick C. Reid 舛屋 圭一

出版者

The Society of Synthetic Organic Chemistry, Japan

雑誌

有機合成化学協会誌 (ISSN:00379980)

巻号頁・発行日

vol.75, no.11, pp.1171-1178, 2017-11-01 (Released:2017-11-09)

参考文献数

51

被引用文献数

34

---

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.