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Issue 28, 2017
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Discovery of a butyrylcholinesterase-specific probe via a structure-based design strategy

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Abstract

We report herein the structure-based design and application of a fluorogenic molecular probe (BChE-FP) specific to butyrylcholinesterase (BChE). This probe was rationally designed by mimicking the native substrate and optimized stepwise by manipulating the steric feature and the reactivity of the designed probe targeting the structural difference of the active pockets of BChE and AChE. The refined probe, BChE-FP, exhibits high specificity toward BChE compared to AChE, producing about 275-fold greater fluorescence enhancement upon the catalysis by BChE. Thus, BChE-FP is a specific BChE probe identified by the structure-based design and it can discriminate BChE from AChE. Furthermore, it has been successfully applied for imaging the endogenous BChE in living cells, as well as BChE inhibitor screening and characterization under physiological conditions.

Graphical abstract: Discovery of a butyrylcholinesterase-specific probe via a structure-based design strategy

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Publication details

The article was received on 25 Jan 2017, accepted on 14 Mar 2017 and first published on 14 Mar 2017


Article type: Communication
DOI: 10.1039/C7CC00577F
Citation: Chem. Commun., 2017,53, 3952-3955
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    Discovery of a butyrylcholinesterase-specific probe via a structure-based design strategy

    S. Yang, Q. Sun, H. Xiong, S. Liu, B. Moosavi, W. Yang and G. Yang, Chem. Commun., 2017, 53, 3952
    DOI: 10.1039/C7CC00577F

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