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Casein Kinase 2 Inhibitor, CX-4945, as a Potential Targeted Anticancer Agent in Gastric Cancer

Authors
 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 
Citation
 ANTICANCER RESEARCH, Vol.38(11) : 6171-6180, 2018 
Journal Title
ANTICANCER RESEARCH
ISSN
 0250-7005 
Issue Date
2018
MeSH
Casein Kinase II/antagonists & inhibitors ; Casein Kinase II/biosynthesis ; Casein Kinase II/genetics ; Cell Line, Tumor ; Humans ; Molecular Targeted Therapy ; Mutation ; Naphthyridines/pharmacology* ; RNA, Messenger/genetics ; RNA, Messenger/metabolism ; Stomach Neoplasms/drug therapy* ; Stomach Neoplasms/enzymology* ; Stomach Neoplasms/genetics
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.
Full Text
http://ar.iiarjournals.org/content/38/11/6171.long
DOI
10.21873/anticanres.12970
Appears in Collections:
1. College of Medicine (의과대학) > Dept. of Internal Medicine (내과학교실) > 1. Journal Papers
Yonsei Authors
Kwon, Woo Sun(권우선) ORCID logo https://orcid.org/0000-0003-0268-5624
Kim, Tae Soo(김태수)
Rha, Sun Young(라선영) ORCID logo https://orcid.org/0000-0002-2512-4531
Park, Kyu Hyun(박규현)
Jung, Min Kyu(정민규) ORCID logo https://orcid.org/0000-0001-8281-3387
Chung, Hyun Cheol(정현철) ORCID logo https://orcid.org/0000-0002-0920-9471
URI
https://ir.ymlib.yonsei.ac.kr/handle/22282913/166694
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