PMID- 29944884
OWN - NLM
STAT- MEDLINE
DCOM- 20181211
LR  - 20220409
IS  - 1090-2104 (Electronic)
IS  - 0006-291X (Linking)
VI  - 503
IP  - 2
DP  - 2018 Sep 5
TI  - The anti-tumor effect of regorafenib in lung squamous cell carcinoma in vitro.
PG  - 1123-1129
LID - S0006-291X(18)31440-2 [pii]
LID - 10.1016/j.bbrc.2018.06.129 [doi]
AB  - Lung squamous cell carcinoma (LSCC) is a common type of non-small-cell lung 
      cancer (NSCLC) and lacks effective treatment. Regorafenib, an oral multikinase 
      inhibitor, has demonstrated promising anti-tumor activity in various solid 
      tumors. To study whether regorafenib inhibits LSCC cells, we investigate the 
      compound in several LSCC cell lines and explore the possible mechanism. In this 
      study, we confirmed that regorafenib had anti-proliferation effect on LSCC cell 
      lines by inducing G0/G1 arrest. In addition, glycogen synthase kinase 3beta (GSK3beta) 
      remained at the same level and Ser9 phosphorylation of GSK3beta decreased with 
      increasing incubation time and increasing regorafenib concentration in LSCC 
      cells. GSK3beta inhibition enhanced the anti-tumor activity of regorafenib. Thus, 
      GSK3beta activation restricted the anti-cancer effect of regorafenib on LSCC. In 
      conclusion, regorafenib might be a promising drug for LSCC therapy. GSK3beta might 
      be a potential target to increase the anti-tumor effect of regorafenib in LSCC 
      cells.
CI  - Copyright (c) 2018 Elsevier Inc. All rights reserved.
FAU - Hu, Xiu
AU  - Hu X
AD  - School of Medicine, Zhejiang University City College, Hangzhou, Zhejiang, 310015, 
      China; College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, 
      Zhejiang, 310058, China.
FAU - Wu, Lin-Wen
AU  - Wu LW
AD  - School of Medicine, Zhejiang University City College, Hangzhou, Zhejiang, 310015, 
      China; College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, 
      Zhejiang, 310058, China.
FAU - Zhang, Zuo-Yan
AU  - Zhang ZY
AD  - School of Medicine, Zhejiang University City College, Hangzhou, Zhejiang, 310015, 
      China; College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, 
      Zhejiang, 310058, China.
FAU - Chen, Meng-Ling
AU  - Chen ML
AD  - School of Medicine, Zhejiang University City College, Hangzhou, Zhejiang, 310015, 
      China.
FAU - Li, Yang-Ling
AU  - Li YL
AD  - Department of Clinical Pharmacology, Affiliated Hangzhou First People's Hospital, 
      Zhejiang University School of Medicine, Hangzhou, Zhejiang, 310006, China. 
      Electronic address: liyangling1215@163.com.
FAU - Zhang, Chong
AU  - Zhang C
AD  - School of Medicine, Zhejiang University City College, Hangzhou, Zhejiang, 310015, 
      China. Electronic address: zhangchong@zucc.edu.cn.
LA  - eng
PT  - Journal Article
PT  - Research Support, Non-U.S. Gov't
DEP - 20180627
PL  - United States
TA  - Biochem Biophys Res Commun
JT  - Biochemical and biophysical research communications
JID - 0372516
RN  - 0 (Antineoplastic Agents)
RN  - 0 (Phenylurea Compounds)
RN  - 0 (Pyridines)
RN  - 24T2A1DOYB (regorafenib)
RN  - EC 2.7.11.1 (Glycogen Synthase Kinase 3 beta)
SB  - IM
MH  - Antineoplastic Agents/*pharmacology
MH  - Carcinoma, Non-Small-Cell Lung/*drug therapy/metabolism/pathology
MH  - Carcinoma, Squamous Cell/drug therapy/metabolism/pathology
MH  - Cell Cycle Checkpoints/drug effects
MH  - Cell Line, Tumor
MH  - Cell Proliferation/drug effects
MH  - Glycogen Synthase Kinase 3 beta/metabolism
MH  - Humans
MH  - Lung Neoplasms/*drug therapy/metabolism/pathology
MH  - Phenylurea Compounds/*pharmacology
MH  - Phosphorylation/drug effects
MH  - Pyridines/*pharmacology
OTO - NOTNLM
OT  - Cell proliferation
OT  - Drug resistance
OT  - GSK3beta
OT  - Lung squamous cell carcinoma
OT  - Regorafenib
EDAT- 2018/06/27 06:00
MHDA- 2018/12/12 06:00
CRDT- 2018/06/27 06:00
PHST- 2018/06/20 00:00 [received]
PHST- 2018/06/22 00:00 [accepted]
PHST- 2018/06/27 06:00 [pubmed]
PHST- 2018/12/12 06:00 [medline]
PHST- 2018/06/27 06:00 [entrez]
AID - S0006-291X(18)31440-2 [pii]
AID - 10.1016/j.bbrc.2018.06.129 [doi]
PST - ppublish
SO  - Biochem Biophys Res Commun. 2018 Sep 5;503(2):1123-1129. doi: 
      10.1016/j.bbrc.2018.06.129. Epub 2018 Jun 27.