Table 2.
Effects of DGAT1/2 inhibitors on tumor cell growth
| Type of tumor | Inhibition of DGATs | Effects on tumor cell growth |
|---|---|---|
| Glioblastoma | DGAT1 inhibitor (A-922500) | Suppressed cell proliferation. Induced cell apoptosis and upregulation of CPT1A protein [96, 104, 105] |
| Inhibition of DGAT1 by shRNA or miRNA-3918 | Increased sensitivity of irradiation and prolonged survival of mice [141] | |
| Melanoma | DGAT1 inhibitors (AZD3988, AZD7687, A922500, or T863) | Suppressed cell proliferation and cell cycle progression. Increased the expression of cleaved caspase-3 protein [121] |
| Gastric cancer | DGAT1 inhibitor (A-922500) | Reduced cell proliferation. Induced apoptosis [147] |
| Prostate cancer | Inhibition of DGAT1 by siRNA or A-922500 | Reduced cell proliferation. Induced of cell cycle G1 arrest and autophagy [122] [116] |
|
Breast cancer (MCF-7 cells) |
DGAT2 inhibitor (PF-06424439) |
Inhibited cell proliferation. Induced cell cycle G2/M arrest. Increased sensitivity of radiation. Reduced cell invasive ability. Reduced LD formation [35, 123, 124] Increased the production of ROS and unrepaired DNA damage of tumor cells after irradiation [123] |
|
Breast cancer (MDA-231 cells) |
DGAT1 inhibitor (A-922500) | Reduced cell proliferation and migratory ability [124] |
| Ovarian cancer | Knockdown of DGAT1 | Inhibited cell proliferation. Reduced cell migration through modulating the EMT process [38] |
| Gastric cancer | Knockdown of DGAT2 | Reduced mesenteric metastatic nodules in the intestinal wall and lung metastasis [39] |
| Colon cancer | DGAT1 inhibitor (A922500) and DGAT2 inhibitor (PF-06424439) | Inhibition of DGAT1 and DGAT2 decreased tumor growth and reduced the proportion of CD206 + MHCII low immunosuppressive myeloid cells in the tumors [150] |