Department of Cellular and Molecular Pharmacology, Juntendo University Graduate School of Medicine, Tokyo, Japan.
Department of Drug Delivery Research, Graduate School of Pharmaceutical Sciences, Kyoto University, Kyoto, Japan.
J Gen Physiol. 2022 Sep 5;154(9). doi: 10.1085/jgp.202112869. Epub 2022 Apr 21.
Type 2 ryanodine receptor (RYR2) is a cardiac Ca2+ release channel in the ER. Mutations in RYR2 are linked to catecholaminergic polymorphic ventricular tachycardia (CPVT). CPVT is associated with enhanced spontaneous Ca2+ release, which tends to occur when [Ca2+]ER reaches a threshold. Mutations lower the threshold [Ca2+]ER by increasing luminal Ca2+ sensitivity or enhancing cytosolic [Ca2+] ([Ca2+]cyt)-dependent activity. Here, to establish the mechanism relating the change in [Ca2+]cyt-dependent activity of RYR2 and the threshold [Ca2+]ER, we carried out cell-based experiments and in silico simulations. We expressed WT and CPVT-linked mutant RYR2s in HEK293 cells and measured [Ca2+]cyt and [Ca2+]ER using fluorescent Ca2+ indicators. CPVT RYR2 cells showed higher oscillation frequency and lower threshold [Ca2+]ER than WT cells. The [Ca2+]cyt-dependent activity at resting [Ca2+]cyt, Arest, was greater in CPVT mutants than in WT, and we found an inverse correlation between threshold [Ca2+]ER and Arest. In addition, lowering RYR2 expression increased the threshold [Ca2+]ER and a product of Arest, and the relative expression level for each mutant correlated with threshold [Ca2+]ER, suggesting that the threshold [Ca2+]ER depends on the net Ca2+ release rate via RYR2. Modeling reproduced Ca2+ oscillations with [Ca2+]cyt and [Ca2+]ER changes in WT and CPVT cells. Interestingly, the [Ca2+]cyt-dependent activity of specific mutations correlated with the age of disease onset in patients carrying them. Our data suggest that the reduction in threshold [Ca2+]ER for spontaneous Ca2+ release by CPVT mutation is explained by enhanced [Ca2+]cyt-dependent activity without requiring modulation of the [Ca2+]ER sensitivity of RYR2.
2 型兰尼碱受体 (RYR2) 是内质网中心肌细胞的 Ca2+释放通道。RYR2 突变与儿茶酚胺多形性室性心动过速 (CPVT) 相关。CPVT 与自发性 Ca2+释放增强有关,这种增强通常发生在内质网 Ca2+浓度达到阈值时。突变通过增加腔室 Ca2+敏感性或增强细胞浆 Ca2+([Ca2+]cyt)依赖性活性来降低阈值 [Ca2+]ER。在这里,为了建立 RYR2 的细胞浆 Ca2+依赖性活性变化与阈值 [Ca2+]ER 之间的关系机制,我们进行了基于细胞的实验和计算机模拟。我们在 HEK293 细胞中表达 WT 和 CPVT 相关的突变型 RYR2,并使用荧光 Ca2+指示剂测量细胞浆 Ca2+([Ca2+]cyt)和内质网 Ca2+([Ca2+]ER)。CPVT RYR2 细胞的振荡频率更高,阈值 [Ca2+]ER 低于 WT 细胞。在静息细胞浆 Ca2+浓度 ([Ca2+]cyt)下,CPVT 突变型的 RYR2 的细胞浆 Ca2+依赖性活性 (Arest)大于 WT 细胞,我们发现阈值 [Ca2+]ER 与 Arest 呈负相关。此外,降低 RYR2 表达会增加阈值 [Ca2+]ER 和 Arest 的乘积,每个突变体的相对表达水平与阈值 [Ca2+]ER 相关,这表明阈值 [Ca2+]ER 取决于通过 RYR2 的净 Ca2+释放率。模型再现了 WT 和 CPVT 细胞中 Ca2+ 振荡与细胞浆 Ca2+浓度和内质网 Ca2+浓度变化之间的关系。有趣的是,特定突变的细胞浆 Ca2+依赖性活性与携带这些突变的患者发病年龄相关。我们的数据表明,CPVT 突变导致自发性 Ca2+释放的阈值 [Ca2+]ER 降低是由于细胞浆 Ca2+依赖性活性增强所致,而无需调节 RYR2 的内质网 Ca2+敏感性。