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丝氨酸水解酶 ABHD6 控制大麻素受体中二酰基甘油(2-AG)的积累和效力。

The serine hydrolase ABHD6 controls the accumulation and efficacy of 2-AG at cannabinoid receptors.

机构信息

Neurobiology and Behavior Graduate Program, University of Washington, Seattle, Washington, USA.

出版信息

Nat Neurosci. 2010 Aug;13(8):951-7. doi: 10.1038/nn.2601. Epub 2010 Jul 25.

Abstract

The endocannabinoid 2-arachidonoylglycerol (2-AG) regulates neurotransmission and neuroinflammation by activating CB1 cannabinoid receptors on neurons and CB2 cannabinoid receptors on microglia. Enzymes that hydrolyze 2-AG, such as monoacylglycerol lipase, regulate the accumulation and efficacy of 2-AG at cannabinoid receptors. We found that the recently described serine hydrolase alpha-beta-hydrolase domain 6 (ABHD6) also controls the accumulation and efficacy of 2-AG at cannabinoid receptors. In cells from the BV-2 microglia cell line, ABHD6 knockdown reduced hydrolysis of 2-AG and increased the efficacy with which 2-AG can stimulate CB2-mediated cell migration. ABHD6 was expressed by neurons in primary culture and its inhibition led to activity-dependent accumulation of 2-AG. In adult mouse cortex, ABHD6 was located postsynaptically and its selective inhibition allowed the induction of CB1-dependent long-term depression by otherwise subthreshold stimulation. Our results indicate that ABHD6 is a rate-limiting step of 2-AG signaling and is therefore a bona fide member of the endocannabinoid signaling system.

摘要

内源性大麻素 2-花生四烯酰甘油(2-AG)通过激活神经元上的 CB1 大麻素受体和小胶质细胞上的 CB2 大麻素受体来调节神经递质传递和神经炎症。水解 2-AG 的酶,如单酰基甘油脂肪酶,调节 2-AG 在大麻素受体上的积累和效力。我们发现,最近描述的丝氨酸水解酶 α-β-水解酶结构域 6(ABHD6)也控制 2-AG 在大麻素受体上的积累和效力。在来自 BV-2 小胶质细胞系的细胞中,ABHD6 的敲低减少了 2-AG 的水解,并增加了 2-AG 刺激 CB2 介导的细胞迁移的效力。ABHD6 在原代培养的神经元中表达,其抑制导致 2-AG 的活性依赖性积累。在成年小鼠大脑皮层中,ABHD6 位于突触后,其选择性抑制允许通过否则亚阈值刺激诱导 CB1 依赖性长时程抑制。我们的结果表明,ABHD6 是 2-AG 信号的限速步骤,因此是内源性大麻素信号系统的真正成员。

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