A focus on the discovery of potent and selective cyclic peptide scaffolds for drug development. Issue 44 (4th November 2022)

• Record Type: Journal Article
• Authors: Saunders, George J.; Yudin, Andrei K.
• Is Part Of: Chemical science. Volume 13:Issue 44(2022)
• Page Start: 12942
• Page End: 12944
• Publication Date: 2022-11-04
• Subjects: Chemistry -- Periodicals; 540.5
• DOI: 10.1039/d2sc90214a
• Languages: English
• ISSNs: 2041-6520

Abstract

Abstract : Library-based screening methods such as mRNA display are paving the way for the discovery of cyclic peptides towards previously undruggable space. Abstract : In the past, cyclic peptide drugs were commonly discovered by isolation of natural products. However, recent efforts predominantly use high-throughput synthetic or genetically encoded libraries to find potent and selective hits against a range of challenging therapeutic targets. Kawamura et al. ( Chem. Sci., 2022, 13, 3256–3262, ; https://doi.org/10.1039/D1SC06844J ) developed a new workflow that can be applied to mRNA display, using high-throughput clustering, SAR investigations and in silico structural studies. This led to the discovery of nanomolar, serum-stable cyclic peptides against the human glucose-dependent insulinotropic peptide receptor (hGIP-R).