Table 2.
Application of STAT3 inhibitors in breast cancer treatment
| Cell Lines | In Vitro or In Vivo | Inhibitors | Radiation | Effects | References |
|---|---|---|---|---|---|
| BT474R/NCI-N87R | In vitro | S3I-201 | NO | Inhibits STAT3 activation and sensitizes resistant cells to trastuzumab treatment | [186] |
| SUM159/BT549 | In vitro/vivo | C188 | NO | Inhibits STAT3 activation (SH2 domain) and ameliorates chemoresistant, like in combining with docetaxel | [187] |
| MDA-MB-231/ 435S | In vitro/vivo | Stattic | NO | Inhibits STAT3 activation, dimerization, and nuclear translocation | [188] |
| MDA-MB-468/ 435/MCF7 | In vitro | STA-21 | NO | Selectively inhibits STAT3 DNA binding capacity and dimerization (did not affect the STAT3 upstream regulators) | [189] |
| 4T1/MCF-7/MDA-MB-231 | In vitro/vivo | Nifuroxazide | NO | Inhibits STAT3 activation, MMP-2/9 expression; decreases MDSCs in lung cancer | [190] |
| MDA-MB-468/231 | In vitro/vivo | Euc | NO | Inhibits STAT3 activation and nuclear translocation | [191] |
| MDA-MB-231/ 468 | In vitro/vivo | DCV | NO | Selectively inhibits STAT3 activation, but does not affect the upstream JAK1/2 and silent STAT3 | [192] |
| MCF-10A/7; | |||||
| MDA-MB-231/468/T47D, | In vitro/vivo | ODZ10117 | NO | Inhibits STAT3 activation (SH2 domain), regardless of other STAT family proteins and upstream regulators | [205] |
| Breast cancer sentinel lymphocyte | In vitro | AG490 | NO | Inhibits the CpG-induced STAT3 activation; promotes DCs maturation and Th1 cells accumulation | [198] |
| 4T1/MDA-MB-231/MCF-7 | In vitro/vivo | Pectolinarigenin | NO | Inhibits STAT3 activation, MMP-2/9 expression; improves CD8+ T cells recruitation | [158] |
| 4T1 | in vitro/vivo | Alisertib | NO | Inhibits STAT3-mediated ROS generation in breast cancer; ameliorates MDSCs immunosuppressive function | [54] |
| TM40D-MB/TUBO | In vitro/vivo | Pyrimethamine (PYR) | NO | Blockes STAT3 activity; decreases the frequencies of Foxp3 + Tregs and promotes the CD8+ T cell | [30] |
| MDA-MB-231/468 | In vitro/vivo | Niclosamide | YES | inhibits STAT3 and Bcl-2, and increases ROS generation in vitro and in vivo; it is identified as a radiosensitizer | [222] |
| SKBR3 | In vitro/vivo | S3I-201 | YES | Inhibits STAT3 activation (radiation-related) and increases radiation-induced cell death | [223] |