Gao M, Ping P, Post S, Insel P A, Tang R, Hammond H K
San Diego Veterans Affairs Medical Center, San Diego, CA 92161, USA.
Proc Natl Acad Sci U S A. 1998 Feb 3;95(3):1038-43. doi: 10.1073/pnas.95.3.1038.
Cellular content of cAMP generated by activation of adenylylcyclase (AC; EC 4.6.1.1) is a key determinant of functional responsiveness in the heart and other tissues. We have tested two hypotheses regarding the relationship between AC content and beta-adrenergic receptor (betaAR)-mediated signal transduction in cardiac myocytes. First, that AC content limits adrenergic signal transduction, and, second, that increased AC, independent of (betaAR) number and G-protein content, yields a proportional increase in betaAR-mediated transmembrane signaling. We used recombinant adenovirus to increase AC isoform VI (ACVI) expression in neonatal cardiac myocytes. Cells that overexpressed ACVI responded to agonist stimulation with marked increases in cAMP production in proportion to protein expressed. In parallel experiments performed on cells transfected with lacZ (control) or ACVI, [3H]forskolin binding, used to assess AC protein expression, was amplified 6-fold, while betaAR-stimulated cAMP production from these cells was increased 7-fold. No changes in betaAR number, or in the heterotrimeric GTP-binding proteins, Galphas or Galphai2, were observed. Previous studies indicate that increased cardiac expression of betaAR or Galphas does not yield proportional increases in transmembrane adrenergic signaling. In contrast, the current data demonstrate that increased ACVI expression provides a proportional increase in beta-adrenergic signal transduction. Our results show that the amount of AC sets a limit on transmembrane beta-adrenergic signaling. We speculate that similar functional responses are possible in other cell types in which AC plays an important physiological role.
由腺苷酸环化酶(AC;EC 4.6.1.1)激活所产生的环磷酸腺苷(cAMP)的细胞含量是心脏和其他组织功能反应性的关键决定因素。我们针对心肌细胞中AC含量与β-肾上腺素能受体(βAR)介导的信号转导之间的关系测试了两种假说。第一种,AC含量限制肾上腺素能信号转导;第二种,AC增加,独立于βAR数量和G蛋白含量,会使βAR介导的跨膜信号转导成比例增加。我们使用重组腺病毒来增加新生心肌细胞中AC同工型VI(ACVI)的表达。过表达ACVI的细胞对激动剂刺激的反应是,cAMP生成量与所表达的蛋白质成比例地显著增加。在用lacZ(对照)或ACVI转染的细胞上进行的平行实验中,用于评估AC蛋白表达的[3H]福斯高林结合增加了6倍,而这些细胞中βAR刺激的cAMP生成增加了7倍。未观察到βAR数量或异三聚体GTP结合蛋白Gαs或Gαi2有变化。先前的研究表明,心脏中βAR或Gαs表达增加并不会使跨膜肾上腺素能信号转导成比例增加。相比之下,当前数据表明,ACVI表达增加会使β-肾上腺素能信号转导成比例增加。我们的结果表明,AC的量对跨膜β-肾上腺素能信号转导设定了限制。我们推测,在AC发挥重要生理作用的其他细胞类型中可能会有类似的功能反应。