Division of Pulmonary and Critical Care Medicine, Joan and Sanford I. Weill Department of Medicine, Weill Cornell Medical College, New York, New York, USA.
Soonchunhyang Institute of Medi-bio Science, Soonchunhyang University, Cheonan-si, Chungcheongnam-do, Republic of Korea.
JCI Insight. 2018 Feb 8;3(3). doi: 10.1172/jci.insight.94979.
Renal fibrosis is a common pathogenic response to injury in chronic kidney disease (CKD). The receptor-interacting protein kinase-3 (RIPK3), a regulator of necroptosis, has been implicated in disease pathogenesis. In mice subjected to unilateral ureteral obstruction-induced (UUO-induced) or adenine diet-induced (AD-induced) renal fibrosis, models of progressive kidney fibrosis, we demonstrate increased kidney expression of RIPK3. Mice genetically deficient in RIPK3 displayed decreased kidney fibrosis and improved kidney function relative to WT mice when challenged with UUO or AD. In contrast, mice genetically deficient in mixed-lineage kinase domain-like protein (MLKL), a downstream RIPK3 target, were not protected from UUO-induced kidney fibrosis. We demonstrate a pathway by which RIPK3 promotes fibrogenesis through the AKT-dependent activation of ATP citrate lyase (ACL). Genetic or chemical inhibition of RIPK3 suppressed the phosphorylation of AKT and ACL in response to TGF-β1 in fibroblasts. Inhibition of AKT or ACL suppressed TGF-β1-dependent extracellular matrix production and myofibroblast differentiation in fibroblasts. Pharmacological inhibition of ACL suppressed UUO-induced kidney fibrosis. RIPK3 expression was highly regulated in human CKD kidney. In conclusion, we identify a pathway by which RIPK3 promotes kidney fibrosis independently of MLKL-dependent necroptosis as a promising therapeutic target in CKD.
肾纤维化是慢性肾脏病(CKD)中损伤的常见致病反应。受体相互作用蛋白激酶-3(RIPK3)是坏死性凋亡的调节剂,与疾病发病机制有关。在单侧输尿管梗阻诱导(UUO 诱导)或腺嘌呤饮食诱导(AD 诱导)的肾纤维化小鼠模型中,我们证明了 RIPK3 在肾脏中的表达增加。与 WT 小鼠相比,缺乏 RIPK3 的基因敲除小鼠在接受 UUO 或 AD 挑战时,肾脏纤维化减少,肾功能改善。相比之下,缺乏混合谱系激酶结构域样蛋白(MLKL)的基因敲除小鼠,RIPK3 的下游靶标,并未免受 UUO 诱导的肾脏纤维化的保护。我们证明了 RIPK3 通过 AKT 依赖性激活三磷酸柠檬酸裂解酶(ACL)促进纤维化的途径。在成纤维细胞中,RIPK3 的基因或化学抑制抑制了 TGF-β1 对 AKT 和 ACL 的磷酸化。AKT 或 ACL 的抑制抑制了成纤维细胞中 TGF-β1 依赖性细胞外基质产生和肌成纤维细胞分化。ACL 的药理学抑制抑制了 UUO 诱导的肾脏纤维化。RIPK3 在人类 CKD 肾脏中的表达受到高度调节。总之,我们确定了 RIPK3 促进肾脏纤维化的途径,该途径独立于 MLKL 依赖性坏死性凋亡,是 CKD 的一个有前途的治疗靶点。