Gao Zhiyong, Young Robert A, Trucco Matteo M, Greene Scott R, Hewlett Erik L, Matschinsky Franz M, Wolf Bryan A
Department of Pathology and Laboratory Medicine, Children's Hospital of Philadelphia and University of Pennsylvania School of Medicine, 5135 Main Building, 34th Street and Civic Center Blvd, Philadelphia, PA 19104-4399, U.S.A.
Biochem J. 2002 Dec 1;368(Pt 2):397-404. doi: 10.1042/BJ20020999.
Activation of protein kinase A (cAMP-dependent protein kinase; PKA) triggers insulin secretion in the beta-cell. Adenylate cyclase toxin (ACT), a bacterial exotoxin with adenylate cyclase activity, and forskolin, an activator of adenylate cyclase, both dose-dependently increased insulin secretion in the presence, but not the absence, of glucose in insulin-secreting betaTC3 cells. The stimulation of cAMP release by either agent was dose-dependent but glucose-independent. Omission of extracellular Ca(2+) totally abolished the effects of ACT on insulin secretion and cytosolic cAMP accumulation. ACT and forskolin caused rapid and dramatic increases in cytosolic Ca(2+), which were blocked by nifedipine and the omission of extracellular Ca(2+). Omission of glucose completely blocked the effects of forskolin and partially blocked the effects of ACT on cytosolic Ca(2+). PKA alpha, beta and gamma catalytic subunits (Calpha, Cbeta and Cgamma respectively) were identified in betaTC6 cells by confocal microscopy. Glucose and glucagon-like polypeptide-1 (GLP-1) caused translocation of Calpha to the nucleus and of Cbeta to the plasma membrane and the nucleus, but did not affect the distribution of Cgamma. In conclusion, glucose and GLP-1 amplify insulin secretion via cAMP production and PKAbeta activation.
蛋白激酶A(环磷酸腺苷依赖性蛋白激酶;PKA)的激活可触发β细胞分泌胰岛素。腺苷酸环化酶毒素(ACT)是一种具有腺苷酸环化酶活性的细菌外毒素,而福斯可林是腺苷酸环化酶的激活剂,在存在葡萄糖而非不存在葡萄糖的情况下,二者均可剂量依赖性地增加胰岛素分泌βTC3细胞的胰岛素分泌。两种试剂对环磷酸腺苷释放的刺激均呈剂量依赖性,但与葡萄糖无关。去除细胞外Ca(2+)可完全消除ACT对胰岛素分泌和胞质环磷酸腺苷积累的影响。ACT和福斯可林可使胞质Ca(2+)迅速显著增加,硝苯地平和去除细胞外Ca(2+)可阻断这种增加。去除葡萄糖可完全阻断福斯可林的作用,并部分阻断ACT对胞质Ca(2+)的作用。通过共聚焦显微镜在βTC6细胞中鉴定出PKAα、β和γ催化亚基(分别为Cα、Cβ和Cγ)。葡萄糖和胰高血糖素样肽-1(GLP-1)可使Cα易位至细胞核,使Cβ易位至质膜和细胞核,但不影响Cγ的分布。总之,葡萄糖和GLP-1通过环磷酸腺苷生成和PKAβ激活来放大胰岛素分泌。