Casein kinase 2 inhibitor, CX-4945, as a potential targeted anticancer agent in gastric cancer

Hyun Myong Kim, Inhye Jeong, Hyun Jeong Kim, Sun Kyoung Kang, Woo Sun Kwon, Tae Soo Kim, Kyu Hyun Park, Minkyu Jung, John Soong, Shu Chuan Lin, Hyuncheol Chung, SunYoung Rha

Research output: Contribution to journalArticle

1 Citation (Scopus)

Abstract

Background/Aim: Casein kinase 2 (CK2) is involved in multiple cellular processes. Furthermore, its overexpression in several human cancers has been associated with tumor progression. In this study, we evaluated the efficacy of the CK2 inhibitor, CX-4945, in gastric cancer cell lines and explored the potential predictive biomarkers for CX-4945 sensitivity. Materials and Methods: The sensitivity to CX-4945 was screened in 49 gastric cancer cell lines by the MTT assay. The mRNA and protein expression of CK2 subunits (α and α') were determined using qRT-PCR and western blot. Furthermore, the activity of CK2α was measured by ELISA. Gene expression and mutations were analyzed via whole-exome and RNA sequencing. Results: The sensitivity to CX-4945 was determined by the inhibition rate (%) at the effective dose (10 μM) which ranged from -1% to 89% in 49 gastric cancer cell lines. CK2α', but not CK2α, mRNA expression was correlated with CX-4945 sensitivity. Conclusion: In this study, CX-4945 showed modest antitumor efficacy in gastric cancer cell lines. CK2 might represent a potential therapeutic target for gastric cancer.

Original languageEnglish
Pages (from-to)6171-6180
Number of pages10
JournalAnticancer research
Volume38
Issue number11
DOIs
Publication statusPublished - 2018 Nov 1

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Casein Kinase II
Antineoplastic Agents
Stomach Neoplasms
Cell Line
Exome
RNA Sequence Analysis
Messenger RNA
5-(3-chlorophenylamino)benzo(c)(2,6)naphthyridine-8-carboxylic acid
Neoplasms
Biomarkers
Western Blotting
Enzyme-Linked Immunosorbent Assay
Gene Expression
Polymerase Chain Reaction
Mutation

All Science Journal Classification (ASJC) codes

  • Oncology
  • Cancer Research

Cite this

Kim, Hyun Myong ; Jeong, Inhye ; Kim, Hyun Jeong ; Kang, Sun Kyoung ; Kwon, Woo Sun ; Kim, Tae Soo ; Park, Kyu Hyun ; Jung, Minkyu ; Soong, John ; Lin, Shu Chuan ; Chung, Hyuncheol ; Rha, SunYoung. / Casein kinase 2 inhibitor, CX-4945, as a potential targeted anticancer agent in gastric cancer. In: Anticancer research. 2018 ; Vol. 38, No. 11. pp. 6171-6180.
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abstract = "Background/Aim: Casein kinase 2 (CK2) is involved in multiple cellular processes. Furthermore, its overexpression in several human cancers has been associated with tumor progression. In this study, we evaluated the efficacy of the CK2 inhibitor, CX-4945, in gastric cancer cell lines and explored the potential predictive biomarkers for CX-4945 sensitivity. Materials and Methods: The sensitivity to CX-4945 was screened in 49 gastric cancer cell lines by the MTT assay. The mRNA and protein expression of CK2 subunits (α and α') were determined using qRT-PCR and western blot. Furthermore, the activity of CK2α was measured by ELISA. Gene expression and mutations were analyzed via whole-exome and RNA sequencing. Results: The sensitivity to CX-4945 was determined by the inhibition rate ({\%}) at the effective dose (10 μM) which ranged from -1{\%} to 89{\%} in 49 gastric cancer cell lines. CK2α', but not CK2α, mRNA expression was correlated with CX-4945 sensitivity. Conclusion: In this study, CX-4945 showed modest antitumor efficacy in gastric cancer cell lines. CK2 might represent a potential therapeutic target for gastric cancer.",
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Kim, HM, Jeong, I, Kim, HJ, Kang, SK, Kwon, WS, Kim, TS, Park, KH, Jung, M, Soong, J, Lin, SC, Chung, H & Rha, S 2018, 'Casein kinase 2 inhibitor, CX-4945, as a potential targeted anticancer agent in gastric cancer', Anticancer research, vol. 38, no. 11, pp. 6171-6180. https://doi.org/10.21873/anticanres.12970

Casein kinase 2 inhibitor, CX-4945, as a potential targeted anticancer agent in gastric cancer. / Kim, Hyun Myong; Jeong, Inhye; Kim, Hyun Jeong; Kang, Sun Kyoung; Kwon, Woo Sun; Kim, Tae Soo; Park, Kyu Hyun; Jung, Minkyu; Soong, John; Lin, Shu Chuan; Chung, Hyuncheol; Rha, SunYoung.

In: Anticancer research, Vol. 38, No. 11, 01.11.2018, p. 6171-6180.

Research output: Contribution to journalArticle

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AU - Jeong, Inhye

AU - Kim, Hyun Jeong

AU - Kang, Sun Kyoung

AU - Kwon, Woo Sun

AU - Kim, Tae Soo

AU - Park, Kyu Hyun

AU - Jung, Minkyu

AU - Soong, John

AU - Lin, Shu Chuan

AU - Chung, Hyuncheol

AU - Rha, SunYoung

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N2 - Background/Aim: Casein kinase 2 (CK2) is involved in multiple cellular processes. Furthermore, its overexpression in several human cancers has been associated with tumor progression. In this study, we evaluated the efficacy of the CK2 inhibitor, CX-4945, in gastric cancer cell lines and explored the potential predictive biomarkers for CX-4945 sensitivity. Materials and Methods: The sensitivity to CX-4945 was screened in 49 gastric cancer cell lines by the MTT assay. The mRNA and protein expression of CK2 subunits (α and α') were determined using qRT-PCR and western blot. Furthermore, the activity of CK2α was measured by ELISA. Gene expression and mutations were analyzed via whole-exome and RNA sequencing. Results: The sensitivity to CX-4945 was determined by the inhibition rate (%) at the effective dose (10 μM) which ranged from -1% to 89% in 49 gastric cancer cell lines. CK2α', but not CK2α, mRNA expression was correlated with CX-4945 sensitivity. Conclusion: In this study, CX-4945 showed modest antitumor efficacy in gastric cancer cell lines. CK2 might represent a potential therapeutic target for gastric cancer.

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