Murrills Richard J, Andrews Jennifer L, Samuel Rachelle L, Coleburn Valerie E, Bhat Bheem M, Bhat Ramesh A, Bex Frederick J, Bodine Peter V N
Department of Osteoporosis & Frailty, Women's Health & Musculoskeletal Biology, Wyeth Research, Collegeville, Pennsylvania 19426, USA.
J Cell Biochem. 2009 Apr 1;106(5):887-95. doi: 10.1002/jcb.22057.
Parathyroid hormone (PTH) activates multiple signaling pathways following binding to the PTH1 receptor in osteoblasts. Previous work revealed a discrepancy between cAMP stimulation and CRE reporter activation of truncated PTH peptides, suggesting that additional signaling pathways contribute to activation of the CRE. Using a CRE-Luciferase reporter containing multiple copies of the CRE stably transfected into the osteoblastic cell line Saos-2, we tested the ability of modulators of alternative pathways to activate the CRE or block the PTH-induced activation of the CRE. Activators of non-cyclic AMP pathways, that is, EGF (Akt, MAPK, JAK/STAT pathways); thapsigargin (intracellular calcium pathway); phorbol myristate acetate (protein kinase C, PKC pathway) induced minor increases in CRE-luciferase activity alone but induced dramatic synergistic effects in combination with PTH. The protein kinase A (PKA) inhibitor H-89 (10 microM) almost completely blocked PTH-induced activation of the CRE-reporter. Adenylate cyclase inhibitors SQ 22536 and DDA had profound and time-dependent biphasic effects on the CRE response. The MAPK inhibitor PD 98059 partially inhibited basal and PTH-induced CRE activity to the same degree, while the PKC inhibitor bisindolylmaleimide (BIS) had variable effects. The calmodulin kinase II inhibitor KN-93 had no significant effect on the response to PTH. We conclude that non-cAMP pathways (EGF pathway, calcium pathway, PKC pathway) converge on, and have synergistic effects on, the response of a CRE reporter to PTH.
甲状旁腺激素(PTH)与成骨细胞中的PTH1受体结合后可激活多种信号通路。先前的研究揭示了截短的PTH肽的cAMP刺激与CRE报告基因激活之间存在差异,这表明其他信号通路也参与了CRE的激活。我们使用稳定转染到成骨细胞系Saos-2中的含有多个CRE拷贝的CRE-荧光素酶报告基因,测试了替代通路调节剂激活CRE或阻断PTH诱导的CRE激活的能力。非环磷酸腺苷(cAMP)通路的激活剂,即表皮生长因子(EGF,Akt、丝裂原活化蛋白激酶(MAPK)、Janus激酶/信号转导子和转录激活子(JAK/STAT)通路);毒胡萝卜素(细胞内钙通路);佛波酯(蛋白激酶C,PKC通路)单独作用时仅引起CRE-荧光素酶活性轻微增加,但与PTH联合作用时则产生显著的协同效应。蛋白激酶A(PKA)抑制剂H-89(10微摩尔)几乎完全阻断了PTH诱导的CRE报告基因激活。腺苷酸环化酶抑制剂SQ 22536和二脱氧腺苷(DDA)对CRE反应具有深刻且时间依赖性的双相作用。MAPK抑制剂PD 98059对基础和PTH诱导的CRE活性具有相同程度的部分抑制作用,而PKC抑制剂双吲哚马来酰胺(BIS)的作用则有所不同。钙调蛋白激酶II抑制剂KN-93对PTH反应无显著影响。我们得出结论,非cAMP通路(EGF通路、钙通路、PKC通路)汇聚并对CRE报告基因对PTH的反应产生协同作用。