Minerva Center for Calcium and Bone Metabolism, Nephrology Services, Hadassah Hebrew University Medical Center, Jerusalem, Israel.
J Clin Invest. 2009 Oct;119(10):3102-14. doi: 10.1172/JCI39522. Epub 2009 Sep 21.
Secondary hyperparathyroidism is a major complication of chronic kidney disease (CKD). In experimental models of secondary hyperparathyroidism induced by hypocalcemia or CKD, parathyroid hormone (PTH) mRNA levels increase due to increased PTH mRNA stability. K-homology splicing regulator protein (KSRP) decreases the stability of PTH mRNA upon binding a cis-acting element in the PTH mRNA 3' UTR region. As the peptidyl-prolyl isomerase (PPIase) Pin1 has recently been shown to regulate the turnover of multiple cytokine mRNAs, we investigated the role of Pin1 in regulating PTH mRNA stability in rat parathyroids and transfected cells. The data generated were consistent with Pin1 being a PTH mRNA destabilizing protein. Initial analysis indicated that Pin1 activity was decreased in parathyroid protein extracts from both hypocalcemic and CKD rats and that pharmacologic inhibition of Pin1 increased PTH mRNA levels posttranscriptionally in rat parathyroid and in transfected cells. Pin1 mediated its effects via interaction with KSRP, which led to KSRP dephosphorylation and activation. In the rat parathyroid, Pin1 inhibition decreased KSRP-PTH mRNA interactions, increasing PTH mRNA levels. Furthermore, Pin1-/- mice displayed increased serum PTH and PTH mRNA levels, suggesting that Pin1 determines basal PTH expression in vivo. These results demonstrate that Pin1 is a key mediator of PTH mRNA stability and indicate a role for Pin1 in the pathogenesis of secondary hyperparathyroidism in individuals with CKD.
继发性甲状旁腺功能亢进症是慢性肾脏病(CKD)的主要并发症。在低钙血症或 CKD 诱导的继发性甲状旁腺功能亢进症的实验模型中,甲状旁腺激素(PTH)mRNA 水平由于 PTH mRNA 稳定性增加而增加。K 同源剪接调节蛋白(KSRP)通过结合 PTH mRNA 3'UTR 区域的顺式作用元件降低 PTH mRNA 的稳定性。最近已经表明,肽基脯氨酰顺反异构酶(Pin1)调节多种细胞因子 mRNA 的周转,因此我们研究了 Pin1 在调节大鼠甲状旁腺和转染细胞中 PTH mRNA 稳定性中的作用。生成的数据与 Pin1 是 PTH mRNA 不稳定蛋白一致。初步分析表明,低钙血症和 CKD 大鼠甲状旁腺蛋白提取物中的 Pin1 活性降低,并且 Pin1 的药理学抑制可在后转录水平增加大鼠甲状旁腺和转染细胞中的 PTH mRNA 水平。Pin1 通过与 KSRP 相互作用发挥其作用,导致 KSRP 去磷酸化和激活。在大鼠甲状旁腺中,Pin1 抑制减少了 KSRP-PTH mRNA 相互作用,增加了 PTH mRNA 水平。此外,Pin1-/- 小鼠显示血清 PTH 和 PTH mRNA 水平增加,表明 Pin1 在体内决定基础 PTH 表达。这些结果表明 Pin1 是 PTH mRNA 稳定性的关键调节剂,并表明 Pin1 在 CKD 个体中继发性甲状旁腺功能亢进症的发病机制中起作用。