In sharp contrast with helical polypeptides carrying basic side chains, Api(8), a basic oligopeptide containing the non-natural achiral amino acid 4-aminopiperidine-4-carboxylic acid (Api), adopts a helical conformation only in acidic media. Alkaline titration of a protonated Api(8) oligomer appended with a leucine derivative at its N-terminus showed that disruption of its helical conformation occurs in a pH range of 7-10. NMR studies indicated that the piperidine groups in Api(8), when nonprotonated, possibly interact with the proximal amide protons in the peptide backbone and hamper the formation of the H-bonding network responsible for the helical conformation. The helical structure is induced not only by protonation but also by acylation of the piperidine groups.
[EN] MODULATORS OF SESTRIN-GATOR2 INTERACTION AND USES THEREOF<br/>[FR] MODULATEURS D'INTERACTION SESTRINE-GATOR2 ET LEURS UTILISATIONS
申请人:NAVITOR PHARM INC
公开号:WO2017070518A1
公开(公告)日:2017-04-27
The present invention provides compounds, compositions thereof, and methods of using the same.