异三聚体G蛋白
5-羟色胺能
细胞生物学
G蛋白
生物
蛋白激酶B
MAPK/ERK通路
RGS2型
受体
信号转导
G蛋白偶联受体
GTPase激活蛋白
血清素
生物化学
作者
Angelique M. Lione,Monica Errico,Stanley L. Lin,David L. Cowen
标识
DOI:10.1046/j.1471-4159.2000.0750934.x
摘要
Abstract: Regulator of G protein signaling (RGS) proteins are GTPase‐activating proteins for heterotrimeric G proteins. One of the best‐studied RGS proteins, RGS4, accelerates the rate of GTP hydrolysis by all G i and G q α subunits yet has been shown to exhibit receptor selectivity. Although RGS4 is expressed primarily in brain, its effect on modulating the activity of serotonergic receptors has not yet been reported. In the present study, transfected BE(2)‐C human neuroblastoma cells expressing human 5‐HT 1B receptors were used to demonstrate that RGS4 can inhibit the coupling of 5‐HT 1B receptors to cellular signals. Serotonin and sumatriptan were found to stimulate activation of extracellular signal‐regulated kinase. This activation was attenuated, but not completely inhibited, by RGS4. Similar inhibition by RGS4 of the protein kinase Akt was also observed. As RGS4 is expressed at high levels in brain, these results suggest that it may play a role in regulating serotonergic pathways.
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