Conformation-locked nucleation strategies ofα-helical peptides
10.13220/j.cnki.jipr.2017.09.007
- VernacularTitle:α-螺旋多肽构象锁定成核策略
- Author:
Ye WU
1
;
Jin-Qiu MO
;
Tai-Rong LIU
;
Hong-Li LIAO
Author Information
1. 成都医学院药学院药化教研室
- Keywords:
protein-protein interactions;
helix;
conformation-restriction;
nucleation;
drug design
- From:
Journal of International Pharmaceutical Research
2017;44(9):860-866
- CountryChina
- Language:Chinese
-
Abstract:
Protein-protein interactions(PPI)with large and shallow interfaces are generally undruggable targets. Many PPI in-volved in vital biological processes are mediated by helixes,therefore PPI can be easily targeted by helical epitope mimics. However, the application of peptide was limited by its conformational flexibility and low stability until the significant work was done by Arora ,et al who applied nucleation and crosslinking strategies to lock peptides in helical conformation. The conformation-locked strategies helps to improve peptide stability,cell permeability,and afterwards target intracellular PPI. At present,the conformation-locked strategies of peptides have achieved great development,and have become a hot spot in peptide research field. In this paper,the recent develop-ment,centering nucleation strategies,applications and bright prospects of helical conformation-locked peptides,are reviewed in order to provide theoretical basis for drug design based on PPI.
