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; 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
, Dik Lung Ma

^*Corresponding author for this work

Department of Chemistry

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

164 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

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.",

keywords = "inhibitors, iridium(III) complexes, metal-based inhibitors, protein-protein interactions, tumor necrosis factor",

author = "Leung, \{Chung Hang\} and Zhong, \{Hai Jing\} and Hui Yang and Zhen Cheng and Chan, \{Daniel Shiu Hin\} and Ma, \{Victor Pui Yan\} and Ruben Abagyan and Wong, \{Chun Yuen\} and Ma, \{Dik Lung\}",

note = "his work is supported by Hong Kong Baptist University (FRG2/10-11/008 and FRG2/11-12/009), Environment and Conservation Fund(ECF Project 3/2010), Centre for Cancer and Inflammation Research, School of Chinese Medicine (CCIR-SCM, HKBU), the Research Fund for the Control of Infectious Diseases (RFCID/11101212), the Research Grants Council (HKBU/201811), and the University of Macau (Start-up Research Grant to C.-H. Leung), MYRG091(Y1-L2)-ICMS12-LCH and MYRG121(Y1-L2)-ICMS12-LCH). ",

year = "2012",

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day = "3",

doi = "10.1002/anie.201202937",

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pages = "9010--9014",

journal = "Angewandte Chemie. International Edition",

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TY - JOUR

T1 - A metal-based inhibitor of tumor necrosis factor-α

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, Dik Lung

N1 - his work is supported by Hong Kong Baptist University (FRG2/10-11/008 and FRG2/11-12/009), Environment and Conservation Fund(ECF Project 3/2010), Centre for Cancer and Inflammation Research, School of Chinese Medicine (CCIR-SCM, HKBU), the Research Fund for the Control of Infectious Diseases (RFCID/11101212), the Research Grants Council (HKBU/201811), and the University of Macau (Start-up Research Grant to C.-H. Leung), MYRG091(Y1-L2)-ICMS12-LCH and MYRG121(Y1-L2)-ICMS12-LCH).

PY - 2012/9/3

Y1 - 2012/9/3

N2 - 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.

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

KW - iridium(III) complexes

KW - metal-based inhibitors

KW - protein-protein interactions

KW - tumor necrosis factor

UR - https://www.scopus.com/pages/publications/84865859280

U2 - 10.1002/anie.201202937

DO - 10.1002/anie.201202937

M3 - Journal article

C2 - 22807261

AN - SCOPUS:84865859280

SN - 1433-7851

VL - 51

SP - 9010

EP - 9014

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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