Inserm, UMR-1048, Institut des Maladies Métaboliques et Cardiovasculaires, F-31342 Toulouse, France.
Cell Signal. 2011 Aug;23(8):1257-66. doi: 10.1016/j.cellsig.2011.03.007. Epub 2011 Mar 22.
Epac proteins respond to the second messenger cyclic AMP (cAMP) and are activated by Gs coupled receptors. They act as specific guanine nucleotide exchange factors (GEFs) for the small G proteins, Rap1 and Rap2 of the Ras family. A plethora of studies using 8-pCPT-2'-O-Me-cAMP, an Epac agonist, has revealed the importance of these multi-domain proteins in the control of key cellular functions such as cell division, migration, growth and secretion. Epac and protein kinase A (PKA) may act independently but are often associated with the same biological process, in which they fulfill either synergistic or opposite effects. In addition, compelling evidence is now accumulating about the formation of molecular complexes in distinct cellular compartments that influence Epac signaling and cellular function. Epac is spatially and temporally regulated by scaffold protein and its effectors are interconnected with other signaling pathways. Pathophysiological changes in Epac signaling may underlie certain diseases.
Epac 蛋白对第二信使环腺苷酸 (cAMP) 作出反应，并被 Gs 偶联受体激活。它们作为 Ras 家族的小 G 蛋白 Rap1 和 Rap2 的特定鸟苷酸交换因子 (GEF) 发挥作用。大量使用 Epac 激动剂 8-pCPT-2'-O-Me-cAMP 的研究揭示了这些多结构域蛋白在控制关键细胞功能（如细胞分裂、迁移、生长和分泌）中的重要性。Epac 和蛋白激酶 A (PKA) 可能独立发挥作用，但通常与相同的生物学过程相关联，在该过程中它们发挥协同或相反的作用。此外，现在有越来越多的证据表明，在不同的细胞区室中形成影响 Epac 信号转导和细胞功能的分子复合物。Epac 通过支架蛋白进行时空调节，其效应物与其他信号通路相互连接。Epac 信号转导的病理生理变化可能是某些疾病的基础。
