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UCP1 激活:利用合成和天然来源的分子治疗肥胖的产热途径中的最热门靶点。

UCP1 activation: Hottest target in the thermogenesis pathway to treat obesity using molecules of synthetic and natural origin.

机构信息

Laboratory of Natural Product Chemistry, Department of Pharmacy, Birla Institute of Technology and Science Pilani, Pilani Campus, Rajasthan 333031, India.

Laboratory of Natural Product Chemistry, Department of Pharmacy, Birla Institute of Technology and Science Pilani, Pilani Campus, Rajasthan 333031, India.

出版信息

Drug Discov Today. 2023 Sep;28(9):103717. doi: 10.1016/j.drudis.2023.103717. Epub 2023 Jul 17.

Abstract

Uncoupling protein 1 (UCP1) has been discovered as a possible target for obesity treatment because of its widespread distribution in the inner mitochondrial membrane of brown adipose tissue (BAT) and high energy expenditure capabilities to burn calories as heat. UCP1 is dormant and does not produce heat without activation as it is inhibited by purine nucleotides. However, activation of UCP1 via either direct interaction with the UCP1 protein, an increase in the expression of UCP1 genes or the physiological production of fatty acids can lead to a rise in the thermogenesis phenomenon. Hence, activation of UCP1 through small molecules of synthetic and natural origin can be considered as a promising strategy to mitigate obesity.

摘要

解偶联蛋白 1(UCP1)因其广泛分布在内线粒体膜的棕色脂肪组织(BAT)和高能量消耗能力以热量形式燃烧卡路里而被发现是肥胖治疗的一个可能靶点。UCP1 是休眠的,在没有被嘌呤核苷酸抑制的情况下不会产生热量。然而,通过与 UCP1 蛋白直接相互作用、增加 UCP1 基因的表达或生理产生脂肪酸来激活 UCP1,可导致产热现象增加。因此,通过合成和天然小分子激活 UCP1 可以被认为是减轻肥胖的一种有前途的策略。

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