Chocarro-Calvo Ana, Zaballos Miguel A, Santisteban Pilar, García-Jiménez Custodia
Facultad de Ciencias de la Salud, Universidad Rey Juan Carlos, Avda de Atenas s/n Alcorcón, Madrid, Spain.
Mol Endocrinol. 2012 Mar;26(3):471-80. doi: 10.1210/me.2011-1309. Epub 2012 Feb 2.
Modulation of MAPK signaling duration by cAMP defines its physiological output by driving cells toward proliferation or differentiation. Understanding how the kinetics of MAPK signaling are integrated with other cellular signals is a key issue in development and cancer. Here we show that dopamine and cAMP-regulated neuronal phosphoprotein, 32 kDa (DARPP-32), a protein required for thyroid cell differentiation, determines whether MAPK/ERK activation is sustained or transient. Serum, a stimulus that activates MAPK signaling and does not independently increase DARPP-32 levels results in transient activation of the MAPK pathway. By contrast, TSH + (IGF-I) activate MAPK signaling but also independently increase DARPP-32 levels. Our results are consistent with a model in which maintenance of DARPP-32 expression by TSH + IGF-I leads to sustained MAPK signaling. Moreover, the sensitivity of MAPK/ERK signaling in thyroid cells is lost when de novo DARPP-32 expression is blocked by small interfering RNA. Because both DARPP-32 levels and function as inhibitor of protein phosphatase 1, a key inhibitor of MAPK kinase activity, are governed by cAMP/protein kinase A, the results may explain why in thyroid cells cAMP signaling downstream from TSH controls the duration of MAPK pathway activity. Thus, fine-tuning of DARPP-32 levels leads to changes in the kinetics or sensitivity of MAPK/ERK signaling. Given the implications of MAPK signaling in thyroid cancer and the loss of DARPP-32 in tumor and transformed thyroid cells, DARPP-32 may represent a key therapeutic target.
环磷酸腺苷(cAMP)对丝裂原活化蛋白激酶(MAPK)信号持续时间的调节通过促使细胞增殖或分化来定义其生理输出。理解MAPK信号动力学如何与其他细胞信号整合是发育和癌症领域的关键问题。在此,我们表明多巴胺和cAMP调节的神经元磷蛋白32 kDa(DARPP - 32),一种甲状腺细胞分化所需的蛋白质,决定了MAPK/细胞外信号调节激酶(ERK)激活是持续的还是短暂的。血清作为一种激活MAPK信号且不会独立增加DARPP - 32水平的刺激物,会导致MAPK途径的短暂激活。相比之下,促甲状腺激素(TSH)+胰岛素样生长因子 - I(IGF - I)激活MAPK信号,但也会独立增加DARPP - 32水平。我们的结果与一个模型一致,即TSH + IGF - I维持DARPP - 32表达会导致MAPK信号持续存在。此外,当小干扰RNA阻断DARPP - 32的从头表达时,甲状腺细胞中MAPK/ERK信号的敏感性丧失。由于DARPP - 32的水平及其作为蛋白磷酸酶1(MAPK激酶活性的关键抑制剂)的功能都受cAMP/蛋白激酶A调控,这些结果可能解释了为什么在甲状腺细胞中TSH下游的cAMP信号控制着MAPK途径活性的持续时间。因此,DARPP - 32水平的微调会导致MAPK/ERK信号动力学或敏感性的变化。鉴于MAPK信号在甲状腺癌中的作用以及肿瘤和转化甲状腺细胞中DARPP - 32的缺失,DARPP - 32可能是一个关键的治疗靶点。