Non-symmetric stapling of native peptides

FJ Chen, W Lin, FE Chen - Nature Reviews Chemistry, 2024 - nature.com
Stapling has emerged as a powerful technique in peptide chemistry. It enables precise
control over peptide conformation leading to enhanced properties such as improved stability …

Synthesis of Membrane-Permeable Macrocyclic Peptides via Imidazopyridinium Grafting

B Li, J Parker, J Tong, T Kodadek - Journal of the American …, 2024 - ACS Publications
Macrocyclic peptides (MPs) are a class of compounds that have been shown to be
particularly well suited for engaging difficult protein targets. However, their utility is limited by …

Origin of Octafluorocyclopentene Polyelectrophilicity

H Tian, W Lee, Y Li, MJ Dweck… - Journal of the …, 2024 - ACS Publications
Octafluorocyclopentene (OFCP) has found utility as a polyelectrophile in substitution
cascades that form complex macrocyclic compounds. The Harran group synthesis of …

A Flow Chemistry Platform for Photochemical Macrocyclization of Peptides

E Morin, W Neiderer, C Cruche, O Bleton… - ACS Sustainable …, 2024 - ACS Publications
The importance of macrocyclic peptides in drug discovery has spawned a variety of modern
techniques to improve their synthesis. Although photocatalysis is now an indispensable tool …

Expedient Synthesis of gem-CF2-2H-Thiophenes from Enaminothiones

X Zhang, X Zhang, R Fu, Z Zhang, Y Jiang - Synlett, 2024 - thieme-connect.com
An expedient and easy-to-handle synthetic platform has been established for the
constructing of 2H-thiophenes carrying fluorine atoms through [4+ 1] cyclization of …