Department of Pharmacology, Rollins Research Center, Emory University School of Medicine, Atlanta, GA 30322, USA.
Mol Pharmacol. 2010 Jun;77(6):1005-15. doi: 10.1124/mol.109.062018. Epub 2010 Mar 9.
The protease-activated receptors (PAR1 and PAR2) are unusual G protein-coupled receptors that are activated by distinct serine proteases and are coexpressed in many different cell types. Limited recent evidence suggests these closely related receptors regulate different physiological outputs in the same cell, although little is known about the comparative signaling pathways used by these receptors. Here we report that PAR1 and PAR2 couple to overlapping and distinct sets of G proteins to regulate receptor-specific signaling pathways involved in cell migration. In functionally PAR-null COS-7 cells, ectopically expressed PAR1 and PAR2 both form stable complexes with G alpha(q), G alpha(11), G alpha(14), G alpha(12), and G alpha(13). It is surprising that PAR1 but not PAR2 coupled to G alpha(o), G alpha(i1), and G alpha(i2). Consistent with these observations, PAR1 and PAR2 stimulation of inositol phosphate production and RhoA activation was blocked by specific inhibitors of G(q/11) and G(12/13) signaling, respectively. Both receptors stimulated extracellular signal-regulated kinase (ERK) 1/2 phosphorylation, but only PAR1 inhibited adenylyl cyclase activity, and pertussis toxin blocked PAR1 effects on both adenylyl cyclase and ERK1/2 signaling. Neu7 astrocytes express native PAR1 and PAR2 receptors that activate inositol phosphate, RhoA, and ERK1/2 signaling. However, only PAR1 inhibited adenylyl cyclase activity. PAR1 and PAR2 also stimulate Neu7 cell migration. PAR1 effects on ERK1/2 phosphorylation and cell migration were blocked both by pertussis toxin and by the mitogen-activated protein kinase kinase/ERK inhibitor [1,4-diamino-2,3-dicyano-1,4-bis(methylthio)butadiene (U0126)], whereas PAR2 effects were only blocked by U0126. These studies demonstrate that PAR1 and PAR2 physically and functionally link to overlapping and distinct profiles of G proteins to differentially regulate downstream signaling pathways and cell physiology.
蛋白酶激活受体 (PAR1 和 PAR2) 是一种不寻常的 G 蛋白偶联受体,它们被不同的丝氨酸蛋白酶激活,并且在许多不同的细胞类型中共同表达。最近的有限证据表明,这些密切相关的受体在同一细胞中调节不同的生理输出,尽管关于这些受体使用的比较信号通路知之甚少。在这里,我们报告 PAR1 和 PAR2 与重叠和不同的 G 蛋白亚基结合,以调节细胞迁移涉及的受体特异性信号通路。在功能上 PAR 缺失的 COS-7 细胞中,异位表达的 PAR1 和 PAR2 都与 G alpha(q)、G alpha(11)、G alpha(14)、G alpha(12)和 G alpha(13)形成稳定的复合物。令人惊讶的是,PAR1 而不是 PAR2 与 G alpha(o)、G alpha(i1)和 G alpha(i2)偶联。这些观察结果一致表明,PAR1 和 PAR2 刺激肌醇磷酸生成和 RhoA 激活分别被 G(q/11)和 G(12/13)信号的特异性抑制剂阻断。两种受体都刺激细胞外信号调节激酶 (ERK) 1/2 磷酸化,但只有 PAR1 抑制腺苷酸环化酶活性,百日咳毒素阻断 PAR1 对腺苷酸环化酶和 ERK1/2 信号的影响。Neu7 星形胶质细胞表达天然的 PAR1 和 PAR2 受体,这些受体激活肌醇磷酸、RhoA 和 ERK1/2 信号。然而,只有 PAR1 抑制腺苷酸环化酶活性。PAR1 和 PAR2 还刺激 Neu7 细胞迁移。PAR1 对 ERK1/2 磷酸化和细胞迁移的影响均被百日咳毒素和丝裂原激活蛋白激酶激酶/ERK 抑制剂 [1,4-二氨基-2,3-二氰基-1,4-双(甲基硫代)丁二烯 (U0126)] 阻断,而 PAR2 的影响仅被 U0126 阻断。这些研究表明,PAR1 和 PAR2 在物理和功能上与重叠和不同的 G 蛋白谱结合,以差异调节下游信号通路和细胞生理学。