Generation of a cell-permeable cycloheptapeptidyl inhibitor against the peptidyl-prolyl isomerase Pin1

被引：15

作者：

Bedewy, Walaa ^{[1
]}

Liao, Hui ^{[1
]}

Abou-Taleb, Nageh A. ^{[2
]}

Hammad, Sherif F. ^{[2
]}

Nasr, Tamer ^{[2
]}

Pei, Dehua ^{[1
]}

机构：

[1] Ohio State Univ, Dept Chem & Biochem, 484 West 12th Ave, Columbus, OH 43210 USA

[2] Helwan Univ, Fac Pharm, Dept Pharmaceut Chem, Helwan, Egypt

来源：

ORGANIC & BIOMOLECULAR CHEMISTRY | 2017年 / 15卷 / 21期

基金：

美国国家卫生研究院;

关键词：

PROTEIN-PROTEIN INTERACTIONS; CANCER-DRIVING PATHWAYS; CYCLIC-PEPTIDES; DISCOVERY; DELIVERY; LIBRARY; DESIGN; GRB2;

D O I：

10.1039/c7ob00430c

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

Cyclic peptides are capable of binding and modulating challenging drug targets including protein-protein interactions. However, their lack of membrane permeability prevents their application against intracellular targets. In this study, we show that it is possible to design a cell-permeable and biologically active cycloheptapeptide inhibitor against the intracellular enzyme peptidyl-prolyl isomerase Pin1 by integrating cell-penetrating and target-binding sequences.

引用

页码：4540 / 4543

页数：4