Department of Biology, University of Rome Tor Vergata, Via della Ricerca Scientifica, 00133, Rome, Italy.
Institute of Translational Pharmacology, CNR, Rome, Italy.
Cell Mol Life Sci. 2021 Feb;78(3):1113-1129. doi: 10.1007/s00018-020-03568-x. Epub 2020 Jun 30.
Protein homeostasis is essential for life in eukaryotes. Organisms respond to proteotoxic stress by activating heat shock transcription factors (HSFs), which play important roles in cytoprotection, longevity and development. Of six human HSFs, HSF1 acts as a proteostasis guardian regulating stress-induced transcriptional responses, whereas HSF2 has a critical role in development, in particular of brain and reproductive organs. Unlike HSF1, that is a stable protein constitutively expressed, HSF2 is a labile protein and its expression varies in different tissues; however, the mechanisms regulating HSF2 expression remain poorly understood. Herein we demonstrate that the proteasome inhibitor anticancer drug bortezomib (Velcade), at clinically relevant concentrations, triggers de novo HSF2 mRNA transcription in different types of cancers via HSF1 activation. Similar results were obtained with next-generation proteasome inhibitors ixazomib and carfilzomib, indicating that induction of HSF2 expression is a general response to proteasome dysfunction. HSF2-promoter analysis, electrophoretic mobility shift assays, and chromatin immunoprecipitation studies unexpectedly revealed that HSF1 is recruited to a heat shock element located at 1.397 bp upstream from the transcription start site in the HSF2-promoter. More importantly, we found that HSF1 is critical for HSF2 gene transcription during proteasome dysfunction, representing an interesting example of transcription factor involved in controlling the expression of members of the same family. Moreover, bortezomib-induced HSF2 was found to localize in the nucleus, interact with HSF1, and participate in bortezomib-mediated control of cancer cell migration. The results shed light on HSF2-expression regulation, revealing a novel level of HSF1/HSF2 interplay that may lead to advances in pharmacological modulation of these fundamental transcription factors.
蛋白质动态平衡对于真核生物的生命至关重要。生物体通过激活热休克转录因子(HSFs)来应对蛋白毒性应激,HSFs 在细胞保护、长寿和发育中发挥着重要作用。在人类的 6 种 HSF 中,HSF1 作为一种蛋白质动态平衡守护者,调节应激诱导的转录反应,而 HSF2 在发育中起着关键作用,特别是在脑和生殖器官的发育中。与稳定表达的 HSF1 不同,HSF2 是一种不稳定的蛋白质,其表达在不同组织中存在差异;然而,调节 HSF2 表达的机制仍知之甚少。本文中,我们证明了蛋白酶体抑制剂抗癌药物硼替佐米(Velcade)在临床相关浓度下,通过 HSF1 激活,在不同类型的癌症中触发新的 HSF2 mRNA 转录。使用下一代蛋白酶体抑制剂 ixazomib 和 carfilzomib 也得到了类似的结果,这表明诱导 HSF2 表达是蛋白酶体功能障碍的普遍反应。HSF2 启动子分析、电泳迁移率变动分析和染色质免疫沉淀研究出人意料地揭示了 HSF1 被招募到 HSF2 启动子中位于转录起始位点上游 1.397bp 的热休克元件上。更重要的是,我们发现 HSF1 在蛋白酶体功能障碍期间对 HSF2 基因转录至关重要,这代表了一种有趣的转录因子参与控制同一家族成员表达的例子。此外,还发现硼替佐米诱导的 HSF2 定位于细胞核内,与 HSF1 相互作用,并参与硼替佐米介导的对癌细胞迁移的控制。这些结果揭示了 HSF2 表达调控的新机制,揭示了 HSF1/HSF2 相互作用的新层面,可能为这些基本转录因子的药理学调节带来新的进展。