A metal-based inhibitor of tumor necrosis factor-α

Chung Hang Leung; Hai Jing Zhong; Hui Yang; Zhen Cheng; Daniel Shiu Hin Chan; Victor Pui Yan Ma; Ruben Abagyan; Chun Yuen Wong; Edmond Dik Lung MA

doi:10.1002/anie.201202937

A metal-based inhibitor of tumor necrosis factor-α

Chung Hang Leung^*, Hai Jing Zhong, Hui Yang, Zhen Cheng, Daniel Shiu Hin Chan, Victor Pui Yan Ma, Ruben Abagyan, Chun Yuen Wong, Edmond Dik Lung MA

^*Corresponding author for this work

Department of Chemistry

Research output: Contribution to journal › Journal article › peer-review

153 Citations (Scopus)

Abstract

Staying in the pocket: A cyclometalated iridium(III) biquinoline complex targets the protein-protein interface (see picture; C yellow, N blue, Ir dark green) of the tumor necrosis factor-α (TNF-α) trimer. Molecular-modeling studies confirm the nature of this interaction. Both enantiomers of the iridium complex display comparable in vitro potency to the strongest small-molecule inhibitor of TNF-α.

Original language	English
Pages (from-to)	9010-9014
Number of pages	5
Journal	Angewandte Chemie. International Edition
Volume	51
Issue number	36
DOIs	https://doi.org/10.1002/anie.201202937
Publication status	Published - 3 Sept 2012

Scopus Subject Areas

Catalysis
Chemistry(all)

User-Defined Keywords

inhibitors
iridium(III) complexes
metal-based inhibitors
protein-protein interactions
tumor necrosis factor

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10.1002/anie.201202937

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title = "A metal-based inhibitor of tumor necrosis factor-α",

abstract = "Staying in the pocket: A cyclometalated iridium(III) biquinoline complex targets the protein-protein interface (see picture; C yellow, N blue, Ir dark green) of the tumor necrosis factor-α (TNF-α) trimer. Molecular-modeling studies confirm the nature of this interaction. Both enantiomers of the iridium complex display comparable in vitro potency to the strongest small-molecule inhibitor of TNF-α.",

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AU - Leung, Chung Hang

AU - Zhong, Hai Jing

AU - Yang, Hui

AU - Cheng, Zhen

AU - Chan, Daniel Shiu Hin

AU - Ma, Victor Pui Yan

AU - Abagyan, Ruben

AU - Wong, Chun Yuen

AU - MA, Edmond Dik Lung

PY - 2012/9/3

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AB - Staying in the pocket: A cyclometalated iridium(III) biquinoline complex targets the protein-protein interface (see picture; C yellow, N blue, Ir dark green) of the tumor necrosis factor-α (TNF-α) trimer. Molecular-modeling studies confirm the nature of this interaction. Both enantiomers of the iridium complex display comparable in vitro potency to the strongest small-molecule inhibitor of TNF-α.

KW - inhibitors

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KW - metal-based inhibitors

KW - protein-protein interactions

KW - tumor necrosis factor

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JO - Angewandte Chemie. International Edition

JF - Angewandte Chemie. International Edition

IS - 36

ER -

A metal-based inhibitor of tumor necrosis factor-α

Abstract

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