Law S F, Yasuda K, Bell G I, Reisine T
Department of Pharmacology and Graduate Group in Cell Biology, University of Pennsylvania, Philadelphia 19104.
J Biol Chem. 1993 May 25;268(15):10721-7.
The interaction of the SRIF receptor subtype SSTR2 with pertussis toxin-sensitive G proteins was investigated using an immunoprecipitation approach employing peptide-directed antisera against Gi alpha and G(o) alpha. Antisera directed against either the COOH terminus of Gi alpha or Go alpha uncoupled SSTR2-G protein complexes from CHO cells stably expressing the cloned receptor indicating that both G proteins form complexes with SSTR2. Chinese hamster ovary cells primarily express Gi alpha 3 and G(o) alpha 2 immunoreactivity, with much lower levels of the other pertussis toxin-sensitive G proteins. Antiserum against Gi alpha 3 uncoupled SSTR2/G protein complexes to a similar extent as Gi alpha common antiserum while antisera against Gi alpha 1 and Gi alpha 2 did not. These findings indicate that SSTR2 expressed in Chinese hamster ovary cells predominantly associates with Gi alpha 3 and G(o) alpha 2. In HEK 293 cells which endogenously express low densities of SSTR2 and similar levels of Gi alpha 1 and Gi alpha 3 immunoreactivity but no G(o) alpha, only antiserum directed against Gi alpha 3 immunoprecipitated SSTR2-G protein complexes, indicating that in these cells SSTR2 primarily associates with Gi alpha 3. SRIF can not inhibit forskolin-stimulated cAMP formation in wild-type HEK 293 cells nor in HEK 293 cells transfected with SSTR2. In contrast, SRIF can inhibit cAMP formation in HEK 293 cells expressing the cloned SRIF receptor SSTR3, which requires the presence of Gi alpha 1 to functionally couple to adenylyl cyclase. The lack of efficient association of SSTR2 with Gi alpha 1 may be the cause of its inability to mediate inhibition of cAMP formation. Differences in the G protein-coupling domains of the cloned SRIF receptors may be responsible for their differences in G protein association and ability to effect various signaling pathways.
利用针对Giα和G(o)α的肽导向抗血清的免疫沉淀方法,研究了生长抑素受体亚型SSTR2与百日咳毒素敏感G蛋白的相互作用。针对Giα或G(o)α羧基末端的抗血清使稳定表达克隆受体的CHO细胞中的SSTR2-G蛋白复合物解偶联,表明这两种G蛋白均与SSTR2形成复合物。中国仓鼠卵巢细胞主要表达Giα3和G(o)α2免疫反应性,其他百日咳毒素敏感G蛋白的水平则低得多。针对Giα3的抗血清与Giα通用抗血清在相似程度上使SSTR2/G蛋白复合物解偶联,而针对Giα1和Giα2的抗血清则不能。这些发现表明,在中国仓鼠卵巢细胞中表达的SSTR2主要与Giα3和G(o)α2相关联。在HEK 293细胞中,内源性表达低密度的SSTR2以及相似水平的Giα1和Giα3免疫反应性,但不表达G(o)α,只有针对Giα3的抗血清能免疫沉淀SSTR2-G蛋白复合物,表明在这些细胞中SSTR2主要与Giα3相关联。生长抑素不能抑制野生型HEK 293细胞或转染了SSTR2的HEK 293细胞中福斯可林刺激的cAMP形成。相比之下,生长抑素可以抑制表达克隆的生长抑素受体SSTR3的HEK 293细胞中的cAMP形成,这需要Giα1的存在才能在功能上与腺苷酸环化酶偶联。SSTR2与Giα1缺乏有效关联可能是其无法介导抑制cAMP形成的原因。克隆的生长抑素受体的G蛋白偶联结构域的差异可能是它们在G蛋白关联和影响各种信号通路能力方面存在差异的原因。