Ebselen as a potent covalent inhibitor of New Delhi metallo-β-lactamase (NDM-1)

Jiachi Chiou; Shengbiao Wan; Kin-Fai Chan; Pui-Kin So; Dandan He; Edward Wai-chi Chan; Tak-Hang Chan; Kwok-Yin Wong; Jiang Tao; Sheng Chen

doi:10.1039/c5cc02594j

Ebselen as a potent covalent inhibitor of New Delhi metallo-β-lactamase (NDM-1)

Jiachi Chiou, Shengbiao Wan, Kin-Fai Chan, Pui-Kin So, Dandan He, Edward Wai-chi Chan, Tak-Hang Chan, Kwok-Yin Wong, Jiang Tao^*, Sheng Chen^*

^*Corresponding author for this work

Research output: Journal Publications and Reviews › RGC 21 - Publication in refereed journal › peer-review

129 Citations (Scopus)

Abstract

We report the discovery of a promising NDM-1 inhibitor, ebselen, through a cell-based screening approach. Enzymatic kinetic study and ESI-MS analysis suggested that ebselen could bind to NDM-1 by forming a S-Se bond with the Cys²²¹ residue at the active site, thereby exhibiting a new inhibition mechanism with broad spectrum inhibitory potential.

Original language	English
Pages (from-to)	9543-9546
Journal	Chemical Communications
Volume	51
Issue number	46
Online published	20 Apr 2015
DOIs	https://doi.org/10.1039/c5cc02594j
Publication status	Published - 11 Jun 2015
Externally published	Yes

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title = "Ebselen as a potent covalent inhibitor of New Delhi metallo-β-lactamase (NDM-1)",

abstract = "We report the discovery of a promising NDM-1 inhibitor, ebselen, through a cell-based screening approach. Enzymatic kinetic study and ESI-MS analysis suggested that ebselen could bind to NDM-1 by forming a S-Se bond with the Cys221 residue at the active site, thereby exhibiting a new inhibition mechanism with broad spectrum inhibitory potential.",

author = "Jiachi Chiou and Shengbiao Wan and Kin-Fai Chan and Pui-Kin So and Dandan He and Chan, {Edward Wai-chi} and Tak-Hang Chan and Kwok-Yin Wong and Jiang Tao and Sheng Chen",

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doi = "10.1039/c5cc02594j",

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T1 - Ebselen as a potent covalent inhibitor of New Delhi metallo-β-lactamase (NDM-1)

AU - Chiou, Jiachi

AU - Wan, Shengbiao

AU - Chan, Kin-Fai

AU - So, Pui-Kin

AU - He, Dandan

AU - Chan, Edward Wai-chi

AU - Chan, Tak-Hang

AU - Wong, Kwok-Yin

AU - Tao, Jiang

AU - Chen, Sheng

PY - 2015/6/11

Y1 - 2015/6/11

N2 - We report the discovery of a promising NDM-1 inhibitor, ebselen, through a cell-based screening approach. Enzymatic kinetic study and ESI-MS analysis suggested that ebselen could bind to NDM-1 by forming a S-Se bond with the Cys221 residue at the active site, thereby exhibiting a new inhibition mechanism with broad spectrum inhibitory potential.

AB - We report the discovery of a promising NDM-1 inhibitor, ebselen, through a cell-based screening approach. Enzymatic kinetic study and ESI-MS analysis suggested that ebselen could bind to NDM-1 by forming a S-Se bond with the Cys221 residue at the active site, thereby exhibiting a new inhibition mechanism with broad spectrum inhibitory potential.

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U2 - 10.1039/c5cc02594j

DO - 10.1039/c5cc02594j

M3 - RGC 21 - Publication in refereed journal

C2 - 25970101

SN - 1359-7345

VL - 51

SP - 9543

EP - 9546

JO - Chemical Communications

JF - Chemical Communications

IS - 46

ER -

Ebselen as a potent covalent inhibitor of New Delhi metallo-β-lactamase (NDM-1)

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