期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 23, 期 18, 页码 5174-5177出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2013.07.011
关键词
Drug discovery; Enzyme inhibitors; Combinatorial chemistry; Ligand separation
资金
- National Key Basic Research Program of China (973 Program) [2012CB725204, 2011CB710803]
- Doctoral Program of Specialized Research Fund [20113221120008]
- Program for Changjiang Scholars and Innovative Research Team in University [IRT1066]
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.
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