scholarly journals The bile acid receptor GPBAR1 (TGR5) is expressed in human gastric cancers and promotes epithelial-mesenchymal transition in gastric cancer cell lines

Oncotarget ◽  
2016 ◽  
Vol 7 (38) ◽  
pp. 61021-61035 ◽  
Author(s):  
Adriana Carino ◽  
Luigina Graziosi ◽  
Claudio D’Amore ◽  
Sabrina Cipriani ◽  
Silvia Marchianò ◽  
...  
2013 ◽  
Vol 134 (10) ◽  
pp. 2373-2382 ◽  
Author(s):  
Tatsuro Watanabe ◽  
Atsushi Takahashi ◽  
Kaori Suzuki ◽  
Miki Kurusu-Kanno ◽  
Kensei Yamaguchi ◽  
...  

2021 ◽  
Vol 12 ◽  
Author(s):  
Peizhi Ma ◽  
Gang Jia ◽  
Zhiyu Song

Lysine-specific demethylase1 (KDM1A) is generally highly expressed in various cancer tissues, and promotes the initiation and development of cancers via diverse cellular signaling pathways. Therefore, KDM1A is a promising drug target in many cancers, and it is crucial to find effective KDM1A inhibitors, while none of them has entered into market. With the help of compound library, monobenzone, a local depigmentor using as a treating over-pigmentation in clinic, was characterized as an effective KDM1A inhibitor (IC50 = 0.4507 μM), which may competitively inhibit KDM1A reversibly. Further cellular study confirmed that monobenzone could inhibit the proliferation of gastric cancer cell lines MGC-803 and BGC-823 with IC50 as 7.82 ± 0.55 μM and 6.99 ± 0.51 μM, respectively, and erase the substrate of KDM1A, H3K4me1/2 and H3K9 me2, and inhibit the migration of gastric cancer cell by reversing epithelial–mesenchymal transition (EMT). As the structure of monobenzone is very simple and small, this study provides a novel backbone for the further optimization of KDM1A inhibitor and gives monobenzone potential new application.


2009 ◽  
Vol 155 (1) ◽  
pp. 40-47 ◽  
Author(s):  
Hideyo Miyato ◽  
Joji Kitayama ◽  
Hiroharu Yamashita ◽  
Daisuke Souma ◽  
Masahiro Asakage ◽  
...  

Oncogene ◽  
2002 ◽  
Vol 21 (42) ◽  
pp. 6549-6556 ◽  
Author(s):  
Jiafu Ji ◽  
Xin Chen ◽  
Suet Yi Leung ◽  
Jen-Tsan A Chi ◽  
Kent Man Chu ◽  
...  

Sign in / Sign up

Export Citation Format

Share Document