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; Hyun Cheol Chung; Sun Young Rha

doi:10.21873/anticanres.12970

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, Hyun Cheol Chung, Sun Young Rha

Department of Internal Medicine

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

12 Citations (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 language	English
Pages (from-to)	6171-6180
Number of pages	10
Journal	Anticancer research
Volume	38
Issue number	11
DOIs	https://doi.org/10.21873/anticanres.12970
Publication status	Published - 2018 Nov

Bibliographical note

Funding Information:
This research was supported by Basic Science Research Program through the National Research Foundation of Korea (NRF) funded by the Ministry of Science, ICT & Future Planning (2017R1A2B2005772) and a grant of the Korea Health Technology R&D Project through the Korea Health Industry Development Institute (KHIDI), funded by the Ministry of Health & Welfare, Republic of Korea (HI13C2096).

Publisher Copyright:
© 2018 International Institute of Anticancer Research.All right reserved.

All Science Journal Classification (ASJC) codes

Oncology
Cancer Research

UN SDGs

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

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10.21873/anticanres.12970

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

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.",

author = "Kim, {Hyun Myong} and Inhye Jeong and Kim, {Hyun Jeong} and Kang, {Sun Kyoung} and Kwon, {Woo Sun} and Kim, {Tae Soo} and Park, {Kyu Hyun} and Minkyu Jung and John Soong and Lin, {Shu Chuan} and Chung, {Hyun Cheol} and Rha, {Sun Young}",

note = "Funding Information: This research was supported by Basic Science Research Program through the National Research Foundation of Korea (NRF) funded by the Ministry of Science, ICT & Future Planning (2017R1A2B2005772) and a grant of the Korea Health Technology R&D Project through the Korea Health Industry Development Institute (KHIDI), funded by the Ministry of Health & Welfare, Republic of Korea (HI13C2096). Publisher Copyright: {\textcopyright} 2018 International Institute of Anticancer Research.All right reserved.",

year = "2018",

month = nov,

doi = "10.21873/anticanres.12970",

language = "English",

volume = "38",

pages = "6171--6180",

journal = "Anticancer Research",

issn = "0250-7005",

publisher = "International Institute of Anticancer Research",

number = "11",

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T1 - Casein kinase 2 inhibitor, CX-4945, as a potential targeted anticancer agent in gastric cancer

AU - Kim, Hyun Myong

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, Hyun Cheol

AU - Rha, Sun Young

N1 - Funding Information: This research was supported by Basic Science Research Program through the National Research Foundation of Korea (NRF) funded by the Ministry of Science, ICT & Future Planning (2017R1A2B2005772) and a grant of the Korea Health Technology R&D Project through the Korea Health Industry Development Institute (KHIDI), funded by the Ministry of Health & Welfare, Republic of Korea (HI13C2096). Publisher Copyright: © 2018 International Institute of Anticancer Research.All right reserved.

PY - 2018/11

Y1 - 2018/11

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.

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

Abstract

Bibliographical note

All Science Journal Classification (ASJC) codes

UN SDGs

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