Effect of sphingomyelinase treatment on ligand binding activity of human serotonin1A receptors.
Effect of sphingomyelinase treatment on ligand binding activity of human serotonin1A receptors.
复制标题
鞘磷脂酶治疗对人血清素 1A 受体配体结合活性的影响。
DOI：
10.1016/j.bbamem.2008.07.007
复制
发表时间：
2008
期刊：
影响因子：
--
通讯作者：
A. Chattopadhyay
中科院分区：
文献类型：
--
作者：
Md. Jafurulla;T. Pucadyil;A. Chattopadhyay
5-羟色胺受体是G蛋白偶联受体家族的重要成员，参与多种认知、行为和发育功能的产生和调节。我们监测了在神经鞘磷脂酶(SMase)处理后，在CHO细胞中稳定表达的人5-羟色胺1A受体(称为CHO-5-HT1AR)的配体结合。神经鞘磷脂酶是一种特异性催化神经酰胺和磷胆碱水解的酶。我们的结果首次表明，鞘磷脂酶处理后，CHO-5-HT1AR细胞膜上5-羟色胺1A受体的特异性配体结合活性增加。饱和结合分析表明，在这些条件下，受体的结合亲和力增加。这伴随着膜有序性的减少，正如完整细胞中膜探针1-[4-(trimethylammonio)phenyl]-6-phenyl-1，3，5-hexatriene(TMA-DPh)的荧光各向异性所监测的那样。这些结果是首次报道鞘磷脂酶处理对这一重要神经递质受体的配体结合活性的影响。
The serotonin1Areceptor is an important member of the G-protein coupled receptor family, and is involved in the generation and modulation of a variety of cognitive, behavioral, and developmental functions. We have monitored the ligand binding of the human serotonin1Areceptor stably expressed in CHO cells (termed CHO-5-HT1AR) following treatment with sphingomyelinase (SMase), an enzyme that specifically catalyzes the hydrolysis of sphingomyelin into ceramide and phosphorylcholine. Our results show, for the first time, that the specific ligand binding activity of the serotonin1Areceptor in membranes isolated from CHO-5-HT1AR cells is increased upon sphingomyelinase treatment. Saturation binding analysis reveals increase in binding affinity of the receptor under these conditions. This is accompanied by a reduction in membrane order, as monitored by fluorescence anisotropy of the membrane probe 1-[4-(trimethylammonio)phenyl]-6-phenyl-1,3,5-hexatriene (TMA-DPH) in intact cells. These results represent the first report on the effect of sphingomyelinase treatment on the ligand binding activity of this important neurotransmitter receptor.
生物膜中的鞘脂组织：模型膜的物理研究揭示了什么。
影响因子：
4
作者：
Brown,RE
通讯作者：
Brown,RE