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

Zheng Fang; Wei He; Xin Li; Zhengjiang Li; Beining Chen; Pingkai Ouyang; Kai Guo

doi:10.1016/j.bmcl.2013.07.011

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

Zheng Fang, Wei He, Xin Li, Zhengjiang Li, Beining Chen, Pingkai Ouyang, Kai Guo

COLLEGE OF BIOTECHNOLOGY AND PHARMACEUTICAL ENGINEERING

Research output: Contribution to journal › Article › peer-review

21 Scopus citations

Abstract

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.

Original language	English
Pages (from-to)	5174-5177
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	23
Issue number	18
DOIs	https://doi.org/10.1016/j.bmcl.2013.07.011
State	Published - 15 Sep 2013

Keywords

Combinatorial chemistry
Drug discovery
Enzyme inhibitors
Ligand separation

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10.1016/j.bmcl.2013.07.011

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Fang, Z., He, W., Li, X., Li, Z., Chen, B., Ouyang, P., & Guo, K. (2013). 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. Bioorganic and Medicinal Chemistry Letters, 23(18), 5174-5177. https://doi.org/10.1016/j.bmcl.2013.07.011

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abstract = "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. Km Data for these new inhibitors was also determined.",

keywords = "Combinatorial chemistry, Drug discovery, Enzyme inhibitors, Ligand separation",

author = "Zheng Fang and Wei He and Xin Li and Zhengjiang Li and Beining Chen and Pingkai Ouyang and Kai Guo",

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Fang, Z , He, W, Li, X, Li, Z, Chen, B, Ouyang, P & Guo, K 2013, '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', Bioorganic and Medicinal Chemistry Letters, vol. 23, no. 18, pp. 5174-5177. https://doi.org/10.1016/j.bmcl.2013.07.011

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. / Fang, Zheng ; He, Wei; Li, Xin et al.
In: Bioorganic and Medicinal Chemistry Letters, Vol. 23, No. 18, 15.09.2013, p. 5174-5177.

Research output: Contribution to journal › Article › peer-review

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T1 - A novel protocol to accelerate dynamic combinatorial chemistry via isolation of ligand-target adducts from dynamic combinatorial libraries

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AU - Fang, Zheng

AU - He, Wei

AU - Li, Xin

AU - Li, Zhengjiang

AU - Chen, Beining

AU - Ouyang, Pingkai

AU - Guo, Kai

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AB - 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. Km Data for these new inhibitors was also determined.

KW - Combinatorial chemistry

KW - Drug discovery

KW - Enzyme inhibitors

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JF - Bioorganic and Medicinal Chemistry Letters

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ER -

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

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Keywords

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