Inhibitory Effect of S1PR2 Antagonist JTE-013 on Proliferation of Chronic Myeloid Leukemia Cells.
10.19746/j.cnki.issn.1009-2137.2020.04.002
- Author:
Meng PANG
1
;
Fang LI
1
;
Jing WANG
1
;
Hong-Mei JING
2
Author Information
1. Department of Hematology, The Third Hospital of Peking University, Beijing 100191, China.
2. Department of Hematology, The Third Hospital of Peking University, Beijing 100191, China,E-mail: hongmei_jing@163.com.
- Publication Type:Journal Article
- MeSH:
Apoptosis;
Cell Proliferation;
Humans;
K562 Cells;
Leukemia, Myelogenous, Chronic, BCR-ABL Positive;
Pyrazoles;
Pyridines;
Receptors, Lysosphingolipid;
Sphingosine-1-Phosphate Receptors
- From:
Journal of Experimental Hematology
2020;28(4):1081-1085
- CountryChina
- Language:Chinese
-
Abstract:
OBJECTIVE:To investigate the effect of sphingosine-1-phosphate receptor 2 (S1PR2) specific antagonist JTE-013 on the proliferation of human chronic myeloid leukemia (CML) cell line K562.
METHODS:K562 cells were treated with JTE-013 (0, 0.5, 1, 5, 10, 20 μmol/L) for 24 and 48 hours respectively, CCK8 assay was used to detect the cell viability. K562 cells were treated with JTE-013 (0, 5, 10, 20 μmol/L) for 24 hours, propidium iodide (PI) DNA staining was used to analyze the cell cycle, Western blot was used to determine the levels of P21 and Cyclin D1 protein expression.
RESULTS:JTE-013 inhibited the proliferation of CML cell line K562 in a dose dependent manner (r=-0.971). The proliferation rate of CML cells showed that the activity of CML cells decreased gradually with the increase of JTE-013 concentration (r=-0.971). The detection demonstrated that JTE-013 suppressed tumor cell proliferation through cell cycle arrest in G/G phase. Further detection of the protein expressions of G phase regulators showed that level of P21 increased, and expression of Cyclin D1 decreased.
CONCLUSION:JTE-013, a S1PR2 antagonist, can inhibit the proliferation of human CML K562 cells, which may be achieved by arresting the cells in G/G phase.
