A small molecule inhibitor of NF-κB, dehydroxymethylepoxyquinomicin (DHMEQ), suppresses growth and invasion of nasopharyngeal carcinoma (NPC) cells

Jason Ho Ting Wong; Vivian Wai Yan Lui; Kazuo Umezawa; Yeung Ho; Elaine Yue Ling Wong; Margaret Heung Ling Ng; Suk Hang Cheng; Chi Man Tsang; Sai Wah Tsao; Anthony Tak Cheung Chan

doi:10.1016/j.canlet.2009.05.022

A small molecule inhibitor of NF-κB, dehydroxymethylepoxyquinomicin (DHMEQ), suppresses growth and invasion of nasopharyngeal carcinoma (NPC) cells

Jason Ho Ting Wong
, Vivian Wai Yan Lui
, Kazuo Umezawa
, Yeung Ho
, Elaine Yue Ling Wong
, Margaret Heung Ling Ng
, Suk Hang Cheng
, Chi Man Tsang
, Sai Wah Tsao
, Anthony Tak Cheung Chan

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

40 Scopus citations

Abstract

Despite the demonstrated constitutive activation of NF-κB in nasopharyngeal carcinoma (NPC), the therapeutic potential of targeting this pathway has not been investigated. Here, we employed a small molecule inhibitor of NF-κB, DHMEQ (which mainly blocks nuclear translocation of activated NF-κB) and demonstrated significant inhibition of NPC cell proliferation, migration, invasion, as well as anchorage-independent growth. These antitumor effects were associated with induction of G₂/M cell cycle arrest and apoptosis, and downregulation of NF-κB target genes (EGFR, cyclin D1 and survivin). This first demonstration of therapeutic benefits of NF-κB targeting in NPC implicates the importance of targeting this pathway in NPC.

Original language	English (US)
Pages (from-to)	23-32
Number of pages	10
Journal	Cancer Letters
Volume	287
Issue number	1
DOIs	https://doi.org/10.1016/j.canlet.2009.05.022
State	Published - Jan 1 2010
Externally published	Yes

Keywords

Anti-invasion
Anti-proliferation
Apoptosis
DHMEQ
Nasopharyngeal carcinoma
NF-κB inhibitor

ASJC Scopus subject areas

Oncology
Cancer Research

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.1016/j.canlet.2009.05.022

Cite this

Wong, J. H. T., Lui, V. W. Y., Umezawa, K., Ho, Y., Wong, E. Y. L., Ng, M. H. L., Cheng, S. H., Tsang, C. M., Tsao, S. W., & Chan, A. T. C. (2010). A small molecule inhibitor of NF-κB, dehydroxymethylepoxyquinomicin (DHMEQ), suppresses growth and invasion of nasopharyngeal carcinoma (NPC) cells. Cancer Letters, 287(1), 23-32. https://doi.org/10.1016/j.canlet.2009.05.022

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title = "A small molecule inhibitor of NF-κB, dehydroxymethylepoxyquinomicin (DHMEQ), suppresses growth and invasion of nasopharyngeal carcinoma (NPC) cells",

abstract = "Despite the demonstrated constitutive activation of NF-κB in nasopharyngeal carcinoma (NPC), the therapeutic potential of targeting this pathway has not been investigated. Here, we employed a small molecule inhibitor of NF-κB, DHMEQ (which mainly blocks nuclear translocation of activated NF-κB) and demonstrated significant inhibition of NPC cell proliferation, migration, invasion, as well as anchorage-independent growth. These antitumor effects were associated with induction of G2/M cell cycle arrest and apoptosis, and downregulation of NF-κB target genes (EGFR, cyclin D1 and survivin). This first demonstration of therapeutic benefits of NF-κB targeting in NPC implicates the importance of targeting this pathway in NPC.",

keywords = "Anti-invasion, Anti-proliferation, Apoptosis, DHMEQ, Nasopharyngeal carcinoma, NF-κB inhibitor",

author = "Wong, \{Jason Ho Ting\} and Lui, \{Vivian Wai Yan\} and Kazuo Umezawa and Yeung Ho and Wong, \{Elaine Yue Ling\} and Ng, \{Margaret Heung Ling\} and Cheng, \{Suk Hang\} and Tsang, \{Chi Man\} and Tsao, \{Sai Wah\} and Chan, \{Anthony Tak Cheung\}",

note = "Funding Information: This study was supported in part by Lee Hysan Foundation Research Grant and Endowment Fund Research Grant from United College, The Chinese University of Hong Kong (CA11117, awarded to VWYL) and a CUHK postdoctoral fellowship scheme (awarded to Y. Ho). Result of this study was presented in part at the Annual Meeting of AACR, 2008. We are grateful to Dr. Cesar Wong for his provision of NPC cell lines and our colleagues for their helpful assistance and advice. ",

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doi = "10.1016/j.canlet.2009.05.022",

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AU - Wong, Jason Ho Ting

AU - Lui, Vivian Wai Yan

AU - Umezawa, Kazuo

AU - Ho, Yeung

AU - Wong, Elaine Yue Ling

AU - Ng, Margaret Heung Ling

AU - Cheng, Suk Hang

AU - Tsang, Chi Man

AU - Tsao, Sai Wah

AU - Chan, Anthony Tak Cheung

N1 - Funding Information: This study was supported in part by Lee Hysan Foundation Research Grant and Endowment Fund Research Grant from United College, The Chinese University of Hong Kong (CA11117, awarded to VWYL) and a CUHK postdoctoral fellowship scheme (awarded to Y. Ho). Result of this study was presented in part at the Annual Meeting of AACR, 2008. We are grateful to Dr. Cesar Wong for his provision of NPC cell lines and our colleagues for their helpful assistance and advice.

PY - 2010/1/1

Y1 - 2010/1/1

N2 - Despite the demonstrated constitutive activation of NF-κB in nasopharyngeal carcinoma (NPC), the therapeutic potential of targeting this pathway has not been investigated. Here, we employed a small molecule inhibitor of NF-κB, DHMEQ (which mainly blocks nuclear translocation of activated NF-κB) and demonstrated significant inhibition of NPC cell proliferation, migration, invasion, as well as anchorage-independent growth. These antitumor effects were associated with induction of G2/M cell cycle arrest and apoptosis, and downregulation of NF-κB target genes (EGFR, cyclin D1 and survivin). This first demonstration of therapeutic benefits of NF-κB targeting in NPC implicates the importance of targeting this pathway in NPC.

AB - Despite the demonstrated constitutive activation of NF-κB in nasopharyngeal carcinoma (NPC), the therapeutic potential of targeting this pathway has not been investigated. Here, we employed a small molecule inhibitor of NF-κB, DHMEQ (which mainly blocks nuclear translocation of activated NF-κB) and demonstrated significant inhibition of NPC cell proliferation, migration, invasion, as well as anchorage-independent growth. These antitumor effects were associated with induction of G2/M cell cycle arrest and apoptosis, and downregulation of NF-κB target genes (EGFR, cyclin D1 and survivin). This first demonstration of therapeutic benefits of NF-κB targeting in NPC implicates the importance of targeting this pathway in NPC.

KW - Anti-invasion

KW - Anti-proliferation

KW - Apoptosis

KW - DHMEQ

KW - Nasopharyngeal carcinoma

KW - NF-κB inhibitor

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AN - SCOPUS:72149129447

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JO - Cancer Letters

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A small molecule inhibitor of NF-κB, dehydroxymethylepoxyquinomicin (DHMEQ), suppresses growth and invasion of nasopharyngeal carcinoma (NPC) cells

Abstract

Keywords

ASJC Scopus subject areas

UN SDGs

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