Brown Foundation Institute of Molecular Medicine for the Prevention of Human Diseases (IMM) University of Texas-Health Science Center at Houston, Houston, Texas, United States of America.
PLoS One. 2013 Aug 2;8(8):e69126. doi: 10.1371/journal.pone.0069126. Print 2013.
BACH2, a B-cell specific transcription factor, plays a critical role in oxidative stress-mediated apoptosis. Bortezomib (Velcade(TM)) is widely used to treat relapsed mantle cell lymphoma (MCL) patients despite varying clinical outcomes. As one of the potential mechanisms of action, bortezomib was reported to elicit endoplasmic reticulum (ER) stress which triggers reactive oxygen species (ROS). In the present study, we investigated the redox-sensitive intracellular mechanism that might play a critical role in bortezomib response in MCL cells. We demonstrated that in MCL cells that are sensitive to bortezomib treatments, BACH2 was translocated to the nucleus in response to bortezomib and induced apoptotic responses through the modulation of anti-oxidative and anti-apoptotic genes. On the other hand, in bortezomib resistant cells, BACH2 expression was confined in the cytoplasm and no suppression of antiapoptotic or antioxidative genes, Nrf2, Gss, CAT, HO-1 and MCL1, was detected. Importantly, levels of BACH2 were significantly higher in bortezomib sensitive MCL patient cells, indicating that BACH2 levels could be an indicator for clinical bortezomib responses. BACH2 translocation to the cytoplasm after phosphorylation was inhibited by PI3K inhibitors and combinatory regimens of bortezomib and PI3K inhibitors sensitized MCL cells to bortezomib. These data suggest that cellular distribution of BACH2 in response to ROS determines the threshold for the induction of apoptosis. Therapies that inhibit BACH2 phosphorylation could be the key for increasing bortezomib cytotoxic response in patients.
BACH2 是一种 B 细胞特异性转录因子,在氧化应激介导的细胞凋亡中发挥关键作用。硼替佐米(万珂)被广泛用于治疗复发性套细胞淋巴瘤(MCL)患者,尽管临床疗效不一。作为潜在的作用机制之一,硼替佐米被报道能引发内质网(ER)应激,从而触发活性氧(ROS)。在本研究中,我们研究了可能在 MCL 细胞对硼替佐米反应中起关键作用的氧化还原敏感的细胞内机制。我们证明,在对硼替佐米治疗敏感的 MCL 细胞中,BACH2 被硼替佐米诱导转移到细胞核,并通过调节抗氧化和抗凋亡基因诱导凋亡反应。另一方面,在硼替佐米耐药细胞中,BACH2 表达局限在细胞质中,未检测到抗凋亡或抗氧化基因(Nrf2、Gss、CAT、HO-1 和 MCL1)的抑制。重要的是,在对硼替佐米敏感的 MCL 患者细胞中,BACH2 水平显著升高,表明 BACH2 水平可作为临床硼替佐米反应的指标。BACH2 在磷酸化后向细胞质的易位被 PI3K 抑制剂和硼替佐米与 PI3K 抑制剂的联合方案抑制,使 MCL 细胞对硼替佐米敏感。这些数据表明,细胞内 BACH2 对 ROS 的反应分布决定了诱导凋亡的阈值。抑制 BACH2 磷酸化的治疗方法可能是增加硼替佐米对患者细胞毒性反应的关键。