Attenuation of ERK/RSK2-driven NFκB gene expression and cancer cell proliferation by kurarinone, a lavandulyl flavanone isolated from Sophora flavescens ait. roots

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Attenuation of ERK/RSK2-driven NFκB gene expression and cancer cell proliferation by kurarinone, a lavandulyl flavanone isolated from Sophora flavescens ait. roots. / Berghe, Wim Vanden; De Naeyer, An; Dijsselbloem, Nathalie; David, Jean-Pierre; De Keukeleire, Denis; Haegeman, Guy.

in: ENDOCR METAB IMMUNE, Jahrgang 11, Nr. 3, 01.09.2011, S. 247-61.

Publikationen: SCORING: Beitrag in Fachzeitschrift/ZeitungSCORING: ZeitschriftenaufsatzForschungBegutachtung

Harvard

Berghe, WV, De Naeyer, A, Dijsselbloem, N, David, J-P, De Keukeleire, D & Haegeman, G 2011, 'Attenuation of ERK/RSK2-driven NFκB gene expression and cancer cell proliferation by kurarinone, a lavandulyl flavanone isolated from Sophora flavescens ait. roots', ENDOCR METAB IMMUNE, Jg. 11, Nr. 3, S. 247-61.

APA

Berghe, W. V., De Naeyer, A., Dijsselbloem, N., David, J-P., De Keukeleire, D., & Haegeman, G. (2011). Attenuation of ERK/RSK2-driven NFκB gene expression and cancer cell proliferation by kurarinone, a lavandulyl flavanone isolated from Sophora flavescens ait. roots. ENDOCR METAB IMMUNE, 11(3), 247-61.

Vancouver

Bibtex

@article{98e263adc02047c48cafbb509cacf5d7,
title = "Attenuation of ERK/RSK2-driven NFκB gene expression and cancer cell proliferation by kurarinone, a lavandulyl flavanone isolated from Sophora flavescens ait. roots",
abstract = "We have analyzed in molecular detail how kurarinone, a lavandulyl flavanone isolated from Sophora flavescens, suppresses nuclear factor-κB (NFκB)-driven interleukin-6 (IL6) expression and cancer cell growth. Interleukin-6 (IL6), involved in cancer-related inflammation, acts as an autocrine and paracrine growth factor, which promotes angiogenesis, metastasis, and subversion of immunity, and changes responsivity to hormones and to chemotherapeutics. Our results in estrogen-unresponsive fibroblasts, ribosomal S6 kinase 2 kinase (RSK2) knockout cells, and estrogen receptor (ER)-deficient breast tumor cells show that kurarinone can inhibit tumor cell proliferation and selectively block nuclear NFκB transactivation of specific target genes such as IL6, cyclin D1, SOD2 but not TNFAIP2. This occurs via attenuation of extracellular signal-regulated protein (ERK) and RSK2 kinase pathways and inhibition of S6 kinase ribosomal protein (S6RP) and histone H3 S10 phosphorylation. As constitutive NFκB and RSK2 activity are important hallmarks of human cancers, including hematopoietic malignancies and solid tumors, prenylated flavanones represent an attractive class of natural inhibitors of the ERK/RSK2 signaling pathway for cancer therapy.",
keywords = "Animals, Breast Neoplasms, Cell Line, Cell Line, Tumor, Cell Proliferation, Extracellular Signal-Regulated MAP Kinases, Female, Flavanones, Flavonoids, Gene Expression Regulation, Enzymologic, Humans, MAP Kinase Signaling System, Mice, Plant Extracts, Plant Roots, Protein-Serine-Threonine Kinases, Ribosomal Protein S6 Kinases, 90-kDa, Sophora",
author = "Berghe, {Wim Vanden} and {De Naeyer}, An and Nathalie Dijsselbloem and Jean-Pierre David and {De Keukeleire}, Denis and Guy Haegeman",
year = "2011",
month = sep,
day = "1",
language = "English",
volume = "11",
pages = "247--61",
journal = "ENDOCR METAB IMMUNE",
issn = "1871-5303",
publisher = "Bentham Science Publishers B.V.",
number = "3",

}

RIS

TY - JOUR

T1 - Attenuation of ERK/RSK2-driven NFκB gene expression and cancer cell proliferation by kurarinone, a lavandulyl flavanone isolated from Sophora flavescens ait. roots

AU - Berghe, Wim Vanden

AU - De Naeyer, An

AU - Dijsselbloem, Nathalie

AU - David, Jean-Pierre

AU - De Keukeleire, Denis

AU - Haegeman, Guy

PY - 2011/9/1

Y1 - 2011/9/1

N2 - We have analyzed in molecular detail how kurarinone, a lavandulyl flavanone isolated from Sophora flavescens, suppresses nuclear factor-κB (NFκB)-driven interleukin-6 (IL6) expression and cancer cell growth. Interleukin-6 (IL6), involved in cancer-related inflammation, acts as an autocrine and paracrine growth factor, which promotes angiogenesis, metastasis, and subversion of immunity, and changes responsivity to hormones and to chemotherapeutics. Our results in estrogen-unresponsive fibroblasts, ribosomal S6 kinase 2 kinase (RSK2) knockout cells, and estrogen receptor (ER)-deficient breast tumor cells show that kurarinone can inhibit tumor cell proliferation and selectively block nuclear NFκB transactivation of specific target genes such as IL6, cyclin D1, SOD2 but not TNFAIP2. This occurs via attenuation of extracellular signal-regulated protein (ERK) and RSK2 kinase pathways and inhibition of S6 kinase ribosomal protein (S6RP) and histone H3 S10 phosphorylation. As constitutive NFκB and RSK2 activity are important hallmarks of human cancers, including hematopoietic malignancies and solid tumors, prenylated flavanones represent an attractive class of natural inhibitors of the ERK/RSK2 signaling pathway for cancer therapy.

AB - We have analyzed in molecular detail how kurarinone, a lavandulyl flavanone isolated from Sophora flavescens, suppresses nuclear factor-κB (NFκB)-driven interleukin-6 (IL6) expression and cancer cell growth. Interleukin-6 (IL6), involved in cancer-related inflammation, acts as an autocrine and paracrine growth factor, which promotes angiogenesis, metastasis, and subversion of immunity, and changes responsivity to hormones and to chemotherapeutics. Our results in estrogen-unresponsive fibroblasts, ribosomal S6 kinase 2 kinase (RSK2) knockout cells, and estrogen receptor (ER)-deficient breast tumor cells show that kurarinone can inhibit tumor cell proliferation and selectively block nuclear NFκB transactivation of specific target genes such as IL6, cyclin D1, SOD2 but not TNFAIP2. This occurs via attenuation of extracellular signal-regulated protein (ERK) and RSK2 kinase pathways and inhibition of S6 kinase ribosomal protein (S6RP) and histone H3 S10 phosphorylation. As constitutive NFκB and RSK2 activity are important hallmarks of human cancers, including hematopoietic malignancies and solid tumors, prenylated flavanones represent an attractive class of natural inhibitors of the ERK/RSK2 signaling pathway for cancer therapy.

KW - Animals

KW - Breast Neoplasms

KW - Cell Line

KW - Cell Line, Tumor

KW - Cell Proliferation

KW - Extracellular Signal-Regulated MAP Kinases

KW - Female

KW - Flavanones

KW - Flavonoids

KW - Gene Expression Regulation, Enzymologic

KW - Humans

KW - MAP Kinase Signaling System

KW - Mice

KW - Plant Extracts

KW - Plant Roots

KW - Protein-Serine-Threonine Kinases

KW - Ribosomal Protein S6 Kinases, 90-kDa

KW - Sophora

M3 - SCORING: Journal article

C2 - 21831037

VL - 11

SP - 247

EP - 261

JO - ENDOCR METAB IMMUNE

JF - ENDOCR METAB IMMUNE

SN - 1871-5303

IS - 3

ER -