Relevance of Peroxisome Proliferator Activated Receptors in Multitarget Paradigm Associated with the Endocannabinoid System.
Relevance of Peroxisome Proliferator Activated Receptors in Multitarget Paradigm Associated with the Endocannabinoid System.
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与内源性大麻素系统相关的多白素范式中过氧化物酶体增殖物激活受体的相关性。
DOI：
10.3390/ijms22031001
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发表时间：
2021-01-20
影响因子：
5.6
通讯作者：
Morales P
中科院分区：
文献类型：
--
作者：
Lago-Fernandez A;Zarzo-Arias S;Jagerovic N;Morales P
大麻素已显示通过多种靶点发挥其治疗作用。这些不仅包括典型的大麻素受体CB 1 R和CB 2 R，还包括相关的孤儿G蛋白偶联受体（GPCR）、配体门控离子通道、瞬时受体电位（TRP）通道、代谢酶和核受体。在这篇综述中，我们的目的是总结报道的化合物表现出其治疗效果的调制CB 1 R和/或CB 2 R和核过氧化物酶体增殖物激活受体（PPARs）。CBR和PPARα或PPARγ亚型的伴随作用已显示介导多种植物源性、内源性和合成大麻素的抗肥胖、镇痛、抗肿瘤或神经保护特性。这种多靶向作用机制的相关性已在不同病理学的背景下进行了分析。还考虑了通过与调节上述靶标的配体的组合治疗引发的协同效应。该文献综述为进一步开发用于特定疾病的双重大麻素提供了结构和药理学见解。
Cannabinoids have shown to exert their therapeutic actions through a variety of targets. These include not only the canonical cannabinoid receptors CB1R and CB2R but also related orphan G protein-coupled receptors (GPCRs), ligand-gated ion channels, transient receptor potential (TRP) channels, metabolic enzymes, and nuclear receptors. In this review, we aim to summarize reported compounds exhibiting their therapeutic effects upon the modulation of CB1R and/or CB2R and the nuclear peroxisome proliferator-activated receptors (PPARs). Concomitant actions at CBRs and PPARα or PPARγ subtypes have shown to mediate antiobesity, analgesic, antitumoral, or neuroprotective properties of a variety of phytogenic, endogenous, and synthetic cannabinoids. The relevance of this multitargeting mechanism of action has been analyzed in the context of diverse pathologies. Synergistic effects triggered by combinatorial treatment with ligands that modulate the aforementioned targets have also been considered. This literature overview provides structural and pharmacological insights for the further development of dual cannabinoids for specific disorders.
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影响因子：
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作者：
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