Molecular neurobiology of the GABAB receptor: Studies of heteromeric receptor function and signalling

抑制性递质γ-氨基丁酸(GABA)的G蛋白偶联受体(GPCR)是一种独特的异源二聚体。将进行分子分析，以深入了解其信号机制和功能调节。利用点突变和嵌合受体的研究将分析配体如何与GABA-BR1亚单位的胞外区域结合，触发G蛋白与GABA-BR2亚单位的细胞内部分的偶联。重点将放在GPCR信号的不同模式上，包括膜和胞质调节蛋白的构成活性和作用。对GABAB受体亚单位的靶向性研究将为GPCR信号的机制调控提供新的信息。

The G protein-coupled receptor (GPCR) for the inhibitory transmitter gamma- aminobutyric acid (GABA) is a unique heterodimer. Molecular analyses will be undertaken to provide insights into its signalling mechanisms and functional regulation. Investigations employing point mutant and chimeric receptors will analyse how ligand binding to the extracellular domain of the GABA-BR1 subunit triggers G protein-coupling to the intracellular portion of the GABA-BR2 subunit. Focus will be on different modes of GPCR signalling, including constitutive activity and roles for membrane and cytosolic regulatory proteins. Targeted studies of GABAB receptor subunits will provide new information on the mechanistic regulation of GPCR signalling.