Division of Medical Oncology, Department of Internal Medicine, Korea University College of Medicine, Korea University, Seoul, 152-703, Republic of Korea; Brain Korea 21 Program for Biomedical Science, Korea University College of Medicine, Korea University, Seoul, 152-703, Republic of Korea.
Division of Medical Oncology, Department of Internal Medicine, Korea University College of Medicine, Korea University, Seoul, 152-703, Republic of Korea.
Cancer Lett. 2019 Apr 10;447:141-153. doi: 10.1016/j.canlet.2019.01.029. Epub 2019 Jan 28.
Triple-negative breast cancer (TNBC) is an aggressive heterogeneous disease with a divergent profile. It has an earlier tendency to form metastases and is associated with poor clinical outcomes due to the limited treatment options available. Heat-shock protein (HSP90) represents a potential treatment target as it promotes tumor progression and metastasis by modulating the maturation and stabilization of signal transduction proteins. We sought to investigate the efficacy of the C-terminal HSP90 inhibitor L80 on cell proliferation, breast cancer stem cell (BCSC)-like properties, tumor growth and metastasis. L80 suppressed cell viability and concomitantly inhibited AKT/MEK/ERK/JAK2/STAT3 signaling in TNBC cells but did not induce cytotoxicity in normal cells. L80 effectively targeted BCSC-like traits, together with significant reductions in the CD44high/CD24low-population, ALDH1 activity and mammosphere forming-ability. In support of the in vitro observations, L80 administration caused significant impairment in tumor growth, angiogenesis and distant metastases in an orthotopic allograft model with BCSC-enriched cells in vivo. These phenomena were associated with the suppression of BCSC-like characteristics and STAT3 dysfunction. Our findings highlight properties of the L80 compound that may be useful in suppressing metastatic TNBC.
三阴性乳腺癌(TNBC)是一种侵袭性异质性疾病,具有不同的特征。它具有更早形成转移的趋势,并由于治疗选择有限而与不良的临床结局相关。热休克蛋白(HSP90)代表了一种潜在的治疗靶点,因为它通过调节信号转导蛋白的成熟和稳定来促进肿瘤的进展和转移。我们试图研究 C 端 HSP90 抑制剂 L80 对细胞增殖、乳腺癌干细胞(BCSC)样特性、肿瘤生长和转移的疗效。L80 抑制了 TNBC 细胞的活力,并同时抑制了 AKT/MEK/ERK/JAK2/STAT3 信号通路,但在正常细胞中没有诱导细胞毒性。L80 有效地靶向 BCSC 样特性,同时显著降低了 CD44high/CD24low 群体、ALDH1 活性和类乳腺球体形成能力。支持体外观察的结果,L80 给药在体内富含 BCSC 的同种异体移植模型中导致肿瘤生长、血管生成和远处转移的显著损害。这些现象与 BCSC 样特性的抑制和 STAT3 功能障碍有关。我们的研究结果突出了 L80 化合物的一些特性,这些特性可能有助于抑制转移性 TNBC。