A novel protocol to accelerate dynamic combinatorial chemistry via isolation of ligand-target adducts from dynamic combinatorial libraries: A case study identifying competitive inhibitors of lysozyme

被引：20

作者：

Fang, Zheng ^{[1
]}

He, Wei ^{[1
]}

Li, Xin ^{[2
]}

Li, Zhengjiang ^{[2
]}

Chen, Beining ^{[3
]}

Ouyang, Pingkai ^{[2
]}

Guo, Kai ^{[2
]}

机构：

[1] Nanjing Univ Technol, Sch Pharmaceut Sci, Nanjing, Jiangsu, Peoples R China

[2] Nanjing Univ Technol, Coll Biotechnol & Pharmaceut Engn, Nanjing, Jiangsu, Peoples R China

[3] Univ Sheffield, Dept Chem, Sheffield S3 7HF, S Yorkshire, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2013年 / 23卷 / 18期

关键词：

Drug discovery; Enzyme inhibitors; Combinatorial chemistry; Ligand separation; IDENTIFICATION; DISCOVERY;

D O I：

10.1016/j.bmcl.2013.07.011

中图分类号：

R914 [药物化学];

学科分类号：

100705 [微生物与生化药学];

摘要：

A novel protocol based on size-exclusion chromatography (SEC) and MS was established to accelerate dynamic combinatorial chemistry (DCC) in this study. By isolating ligand-target adducts from the dynamic combinatorial library (DCL), ligands could be identified directly by MS after denaturation. Three new inhibitors for lysozyme were discovered by this SEC-MS protocol in a case study. K-m Data for these new inhibitors was also determined. (C) 2013 Elsevier Ltd. All rights reserved.

引用

页码：5174 / 5177

页数：4

共 25 条

[1]

Exploring the differential recognition of DNA G-quadruplex targets by small molecules using dynamic combinatorial chemistry [J].