Peptide-Assisted Enhancement of Inhibitory Effects of Small Molecular Inhibitors for Kinases

被引：3
|
作者：
Wang, Wei [1 ,4 ]
Hirano, Yoshinori [2 ]
Uzawa, Takanori [1 ,3 ]
Taiji, Makoto [2 ]
Ito, Yoshihiro [1 ,3 ]
机构：
[1] RIKEN, Nano Med Engn Lab, 2-1 Hirosawa, Wako, Saitama 3510198, Japan
[2] RIKEN, Quantitat Biol Ctr, Lab Computat Mol Design, Computat Biol Res Core,Chou Ku, 1-6-5 Minatojima Minamimachi, Kobe, Hyogo 6500047, Japan
[3] RIKEN, Ctr Emergent Matter Sci, Emergent Bioengn Mat Res Team, 2-1 Hirosawa, Wako, Saitama 3510198, Japan
[4] Chinese Acad Sci, High Field Magnet Lab, Hefei 230031, Anhui, Peoples R China
来源：
BULLETIN OF THE CHEMICAL SOCIETY OF JAPAN | 2016年 / 89卷 / 04期
基金：
日本学术振兴会;
关键词：
IN-VITRO SELECTION; APTAMER; RNA; RECOGNITION; LIBRARY; DESIGN;
D O I：
10.1246/bcsj.20150414
中图分类号：
O6 [化学];
学科分类号：
0703 ;
摘要：
Conjugation of small molecular inhibitor with a site recognition peptide would generate highly potent peptide drug conjugate inhibitors of protein kinases. A peptide selected by ribosome display with a tRNA carrying an inhibitor conjugated amino acid exhibited up to 10- to 100-fold higher inhibitory effects towards different kinases than solely the inhibitor.
引用
收藏
页码：444 / 446
页数：3
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