Zhu Chenggang, Huang Haishan, Hua Rongsheng, Li Guo, Yang Dong, Luo Jiansong, Zhang Cunxin, Shi Liangen, Benovic Jeffrey L, Zhou Naiming
Institute of Biochemistry, College of Life Sciences, Zijingang Campus, Zhejiang University, Hangzhou, Zhejiang 310058, China.
FEBS Lett. 2009 May 6;583(9):1463-8. doi: 10.1016/j.febslet.2009.03.060. Epub 2009 Apr 2.
Neuropeptides of the adipokinetic hormone (AKH) family are among the best studied hormone peptides, but its signaling pathways remain to be elucidated. In this study, we molecularly characterized the signaling of Bombyx AKH receptor (AKHR) and its peptide ligands in HEK293 cells. In HEK293 cells stably expressing AKHR, AKH1 stimulation not only led to a ligand concentration dependent mobilization of intracellular Ca(2+) and cAMP accumulation, but also elicited transient activation of extracellular signal-regulated kinase 1/2 (ERK1/2) pathway. We observed that AKH receptor was rapidly internalized after AKH1 stimulation. We further demonstrated that AKH2 exhibited high activities in cAMP accumulation and ERK1/2 activation on AKHR comparable to AKH1, whereas AKH3 was much less effective.
脂肪动激素(AKH)家族的神经肽是研究最为深入的激素肽之一,但其信号通路仍有待阐明。在本研究中,我们对家蚕AKH受体(AKHR)及其肽配体在HEK293细胞中的信号传导进行了分子特征分析。在稳定表达AKHR的HEK293细胞中,AKH1刺激不仅导致细胞内Ca(2+)的配体浓度依赖性动员和cAMP积累,还引发细胞外信号调节激酶1/2(ERK1/2)途径的瞬时激活。我们观察到,AKH1刺激后AKH受体迅速内化。我们进一步证明,AKH2在cAMP积累和ERK1/2激活方面对AKHR表现出与AKH1相当的高活性,而AKH3的效果则差得多。