University of Chinese Academy of Sciences, No.19A Yuquan Road, Beijing, 100049, China; Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zuchongzhi Road, Pudong, Shanghai, 201203, China; School of Life Science and Technology, ShanghaiTech University, 393 Middle Huaxia Road, Pudong, Shanghai, 201210, China.
Shanghai Center for Systems Biomedicine, Shanghai Jiao Tong University, 800 Dong Chuan Rd, Minhang, Shanghai, 200240, China.
Biochem Biophys Res Commun. 2018 Sep 3;503(1):249-256. doi: 10.1016/j.bbrc.2018.06.010. Epub 2018 Jun 15.
Malignant melanoma has shown increased incidence and high mortality rate in the last three decades. In this study, we investigated whether combination therapy with ch282-5 (a novel BH3 mimetic) and microwave hyperthermia could display synergistic antitumor effects against melanoma. Our results indicated that combination therapy reduced the viability and proliferation of melanoma cells. Through inhibiting the expression of anti-apoptotic proteins of Bcl-2 and IAP family and activating MAPK proteins, combined hyperthermia enhanced ch282-5-induced apoptosis. Combination therapy also synergistically disturbed the mTOR/p70S6k signaling pathway, which is important for cell survival and migration. Moreover, our results showed that combination therapy remarkably suppressed melanoma cell migration in vitro and significantly reduced experimental pulmonary metastasis in vivo. In conclusion, our results indicate that combination therapy with ch282-5 and hyperthermia has synergistic antitumor effects and provides a possible therapeutic strategy for advanced melanoma.
在过去的三十年中,恶性黑色素瘤的发病率和死亡率均呈上升趋势。在这项研究中,我们研究了新型 BH3 模拟物 ch282-5 与微波热疗联合治疗是否对黑色素瘤具有协同抗肿瘤作用。我们的结果表明,联合治疗可降低黑色素瘤细胞的活力和增殖。通过抑制抗凋亡蛋白 Bcl-2 和 IAP 家族的表达以及激活 MAPK 蛋白,联合热疗增强了 ch282-5 诱导的细胞凋亡。联合治疗还协同扰乱了 mTOR/p70S6k 信号通路,该通路对细胞存活和迁移很重要。此外,我们的结果表明,联合治疗可显著抑制黑色素瘤细胞在体外的迁移,并显著减少体内实验性肺转移。总之,我们的结果表明,ch282-5 与热疗联合治疗具有协同抗肿瘤作用,为晚期黑色素瘤提供了一种可能的治疗策略。