Müller Rolf
Institute of Molecular Biology and Tumor Research, Center for Tumor Biology and Immunology, Philipps University, Hans-Meerwein-Str. 3, 35043 Marburg, Germany.
Biochimie. 2017 May;136:90-99. doi: 10.1016/j.biochi.2016.10.019. Epub 2016 Dec 2.
The nuclear receptor factor peroxisome proliferator-activated receptor (PPARβ/δ) can regulate its target genes by transcriptional activation or repression through both ligand-dependent and independent mechanism as well as by interactions with other transcription factors. PPARβ/δ exerts essential regulatory functions in intermediary metabolism that have been elucidated in detail, but clearly also plays a role in inflammation, differentiation, apoptosis and other cancer-associated processes, which is, however, mechanistically only partly understood. Consistent with these functions clinical associations link the expression of PPARβ/δ and its target genes to an unfavorable outcome of several human cancers. However, the available data do not yield a clear picture of PPARβ/δ's role in cancer-associated processes and are in fact partly controversial. This article provides an overview of this research area and discusses the role of PPARβ/δ in cancer in light of the complex mechanisms of its transcriptional regulation and its potential as a druggable anti-cancer target.
核受体因子过氧化物酶体增殖物激活受体（PPARβ/δ）可通过配体依赖性和非依赖性机制以及与其他转录因子的相互作用，通过转录激活或抑制来调控其靶基因。PPARβ/δ在中间代谢中发挥着重要的调节功能，这一点已得到详细阐明，但它显然也在炎症、分化、凋亡及其他与癌症相关的过程中发挥作用，不过，其作用机制仅部分为人所知。与这些功能一致的是，临床关联将PPARβ/δ及其靶基因的表达与多种人类癌症的不良预后联系起来。然而，现有数据并未清晰呈现PPARβ/δ在癌症相关过程中的作用，实际上部分数据还存在争议。本文对该研究领域进行了综述，并鉴于PPARβ/δ转录调控的复杂机制及其作为可成药抗癌靶点的潜力，探讨了其在癌症中的作用。
