Beijing Key Laboratory of Gene Resource and Molecular Development, College of Life Sciences, Beijing Normal University, Beijing 100875, China.
Key Laboratory for Cell Proliferation and Regulation Biology of State Education Ministry, College of Life Sciences, Beijing Normal University, Beijing 100875, China.
Molecules. 2019 Jul 12;24(14):2545. doi: 10.3390/molecules24142545.
It has been more than 36 years since peroxisome proliferator-activated receptors (PPARs) were first recognized as enhancers of peroxisome proliferation. Consequently, many studies in different fields have illustrated that PPARs are nuclear receptors that participate in nutrient and energy metabolism and regulate cellular and whole-body energy homeostasis during lipid and carbohydrate metabolism, cell growth, cancer development, and so on. With increasing challenges to human health, PPARs have attracted much attention for their ability to ameliorate metabolic syndromes. In our previous studies, we found that the complex functions of PPARs may be used as future targets in obesity and atherosclerosis treatments. Here, we review three types of PPARs that play overlapping but distinct roles in nutrient and energy metabolism during different metabolic states and in different organs. Furthermore, research has emerged showing that PPARs also play many other roles in inflammation, central nervous system-related diseases, and cancer. Increasingly, drug development has been based on the use of several selective PPARs as modulators to diminish the adverse effects of the PPAR agonists previously used in clinical practice. In conclusion, the complex roles of PPARs in metabolic networks keep these factors in the forefront of research because it is hoped that they will have potential therapeutic effects in future applications.
过氧化物酶体增殖物激活受体 (PPARs) 最初被发现能够增强过氧化物酶体增殖，距今已有 36 多年。因此，不同领域的许多研究表明，PPARs 是核受体，参与营养和能量代谢，并在脂质和碳水化合物代谢、细胞生长、癌症发展等过程中调节细胞和全身能量稳态。随着人类健康面临的挑战不断增加，PPARs 因其改善代谢综合征的能力而备受关注。在我们之前的研究中，我们发现 PPARs 的复杂功能可能被用作肥胖和动脉粥样硬化治疗的未来靶点。在这里，我们综述了三种类型的 PPARs，它们在不同代谢状态和不同器官中的营养和能量代谢中发挥重叠但又不同的作用。此外，研究还表明，PPARs 在炎症、中枢神经系统相关疾病和癌症中也发挥着许多其他作用。越来越多的药物开发基于使用几种选择性 PPAR 作为调节剂来减少以前在临床实践中使用的 PPAR 激动剂的不良反应。总之，PPARs 在代谢网络中的复杂作用使这些因素成为研究的前沿，因为人们希望它们在未来的应用中具有潜在的治疗效果。
