Graduate School of Life and Environmental Sciences, University of Tsukuba, Tennoudai 1-1-1, Tsukuba 305-8572, Japan.
PPAR Res. 2013;2013:109285. doi: 10.1155/2013/109285. Epub 2013 Feb 3.
PPARs are ligand activated transcription factors. PPARγ agonists have been reported as a new and potentially efficacious treatment of inflammation, diabetes, obesity, cancer, AD, and schizophrenia. Since cancer cells show dysregulation of glycolysis they are potentially manageable through changes in metabolic environment. Interestingly, several of the genes involved in maintaining the metabolic environment and the central energy generation pathway are regulated or predicted to be regulated by PPARγ. The use of synthetic PPARγ ligands as drugs and their recent withdrawal/restricted usage highlight the lack of understanding of the molecular basis of these drugs, their off-target effects, and their network. These data further underscores the complexity of nuclear receptor signalling mechanisms. This paper will discuss the function and role of PPARγ in energy metabolism and cancer biology in general and its emergence as a promising therapeutic target in breast cancer.
过氧化物酶体增殖物激活受体(PPARs)是配体激活的转录因子。有报道称,PPARγ 激动剂是一种新的、有潜在疗效的治疗炎症、糖尿病、肥胖症、癌症、AD 和精神分裂症的药物。由于癌细胞的糖酵解出现失调,因此通过改变代谢环境,这些癌细胞可能是可以控制的。有趣的是,参与维持代谢环境和中央能量生成途径的几个基因受到 PPARγ 的调节或预测受到其调节。合成的 PPARγ 配体作为药物的使用及其最近的撤回/限制使用突出表明,人们对这些药物的分子基础、脱靶效应及其网络缺乏了解。这些数据进一步强调了核受体信号转导机制的复杂性。本文将讨论 PPARγ 在能量代谢和癌症生物学中的一般功能和作用,以及其作为乳腺癌有前途的治疗靶点的出现。