Department of Molecular and Integrative Physiology, University of Michigan Medical School, Ann Arbor, Michigan;
Department of Radiology, University of Michigan Medical School, Ann Arbor, Michigan;
Am J Physiol Gastrointest Liver Physiol. 2014 Oct 1;307(7):G700-10. doi: 10.1152/ajpgi.00163.2014. Epub 2014 Aug 7.
High levels of cholecystokinin (CCK) can stimulate pancreatic adaptive growth in which mature acinar cells divide, leading to enhanced pancreatic mass with parallel increases in protein, DNA, RNA, and digestive enzyme content. Prolonged release of CCK can be induced by feeding trypsin inhibitor (TI) to disrupt normal feedback control. This leads to exocrine growth in a CCK-dependent manner. The extracellular signal-related kinase (ERK) pathway regulates many proliferative processes in various tissues and disease models. The aim of this study was to evaluate the role of ERK signaling in pancreatic adaptive growth using the MEK inhibitors PD-0325901 and trametinib (GSK-1120212). It was determined that PD-0325901 given two times daily by gavage or mixed into powdered chow was an effective and specific inhibitor of ERK signaling in vivo. TI-containing chow led to a robust increase in pancreatic mass, protein, DNA, and RNA content. This pancreatic adaptive growth was blocked in mice fed chow containing the MEK inhibitors. PD-0325901 blocked TI-induced ERK-regulated early response genes, cell-cycle proteins, and mitogenesis by acinar cells. It was determined that ERK signaling is necessary for the initiation of pancreatic adaptive growth but not necessary to maintain it. PD-0325901 blocked adaptive growth when given before cell-cycle initiation but not after mitogenesis had been established. Furthermore, GSK-1120212, a chemically distinct inhibitor of the ERK pathway that is now approved for clinical use, inhibited growth similar to PD-0325901. These data demonstrate that the ERK pathway is required for CCK-stimulated pancreatic adaptive growth.
胆囊收缩素 (CCK) 水平升高可刺激胰腺适应性生长,使成熟的腺泡细胞分裂,导致胰腺质量增加,同时蛋白质、DNA、RNA 和消化酶含量也增加。通过给予胰蛋白酶抑制剂 (TI) 来破坏正常的反馈控制,可以长时间释放 CCK。这导致以 CCK 依赖性方式发生外分泌生长。细胞外信号相关激酶 (ERK) 途径调节各种组织和疾病模型中的许多增殖过程。本研究旨在使用 MEK 抑制剂 PD-0325901 和 trametinib (GSK-1120212) 评估 ERK 信号在胰腺适应性生长中的作用。结果表明,通过灌胃或混入粉末饲料每日两次给予 PD-0325901 是体内 ERK 信号的有效和特异性抑制剂。含 TI 的饲料导致胰腺质量、蛋白质、DNA 和 RNA 含量的显著增加。用含有 MEK 抑制剂的饲料喂养的小鼠中,这种胰腺适应性生长被阻断。PD-0325901 阻断了 TI 诱导的 ERK 调节的早期反应基因、细胞周期蛋白和腺泡细胞的有丝分裂。研究结果表明,ERK 信号对于胰腺适应性生长的启动是必需的,但对于维持它是不必要的。PD-0325901 在细胞周期开始之前给予时可阻断适应性生长,但在有丝分裂已经建立后给予则不能。此外,GSK-1120212 是一种化学上不同的 ERK 途径抑制剂,目前已获准用于临床,其对生长的抑制作用类似于 PD-0325901。这些数据表明,ERK 途径是 CCK 刺激的胰腺适应性生长所必需的。