Sandra Hummelgaard, Jean-Claude Kresse, Michael Schou Jensen, Simon Glerup, Kathrin Weyer
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Recent findings indicate that PCSK9 aggravates proteinuria by interacting with and downregulating megalin, a proximal tubule receptor essential for protein reabsorption in the kidney. Inhibition of PCSK9 has been shown to preserve megalin levels, reduce proteinuria, and improve the disease phenotype in experimental models. However, conflicting data from preclinical studies underscore the need for further research to clarify the mechanisms underlying PCSK9's role in kidney disease. 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引用次数: 0
摘要
慢性肾脏疾病(CKD)是心血管疾病(CVD)的重要危险因素。CKD的主要特征包括蛋白尿和肾小球滤过率降低,这两者都与疾病进展和不良结局有关。血脂异常是一种主要的心血管疾病危险因素,通常与CKD严重程度相关,传统治疗方法不能充分解决这一问题。蛋白转化酶subtilisin/ keexin type 9 (PCSK9)通过调节低密度脂蛋白受体(LDLR)水平在脂质代谢中起关键作用,并已成为控制血脂异常的治疗靶点。PCSK9抑制剂,包括单克隆抗体和siRNA,有效降低LDL胆固醇水平,并已证明在轻度至中度CKD患者中的安全性。最近的研究结果表明,PCSK9通过与巨噬蛋白相互作用并下调巨噬蛋白,从而加重蛋白尿,巨噬蛋白是肾脏中蛋白质重吸收所必需的近端小管受体。在实验模型中,抑制PCSK9已被证明可以保持巨噬细胞蛋白水平,减少蛋白尿,并改善疾病表型。然而,来自临床前研究的相互矛盾的数据强调需要进一步研究来阐明PCSK9在肾脏疾病中的作用机制。本综述强调了PCSK9抑制在CKD中治疗蛋白尿和血脂异常的潜力,强调了其作为一种治疗策略的前景,同时指出了当前的挑战和未来的研究方向。
Emerging roles of PCSK9 in kidney disease: lipid metabolism, megalin regulation and proteinuria.
Chronic kidney disease (CKD) is a significant risk factor for cardiovascular disease (CVD). Key features of CKD include proteinuria and reduced glomerular filtration rate, both of which are linked to disease progression and adverse outcomes. Dyslipidemia, a major CVD risk factor, often correlates with CKD severity and is inadequately addressed by conventional therapies. Proprotein convertase subtilisin/kexin type 9 (PCSK9) plays a critical role in lipid metabolism by modulating low-density lipoprotein receptor (LDLR) levels and has emerged as a therapeutic target for managing dyslipidemia. PCSK9 inhibitors, including monoclonal antibodies and siRNA, effectively lower LDL cholesterol levels and have demonstrated safety in patients with mild to moderate CKD. Recent findings indicate that PCSK9 aggravates proteinuria by interacting with and downregulating megalin, a proximal tubule receptor essential for protein reabsorption in the kidney. Inhibition of PCSK9 has been shown to preserve megalin levels, reduce proteinuria, and improve the disease phenotype in experimental models. However, conflicting data from preclinical studies underscore the need for further research to clarify the mechanisms underlying PCSK9's role in kidney disease. This review highlights the potential of PCSK9 inhibition in addressing proteinuria and dyslipidemia in CKD, emphasizing its promise as a therapeutic strategy, while addressing current challenges and future directions for research.
期刊介绍:
Pflügers Archiv European Journal of Physiology publishes those results of original research that are seen as advancing the physiological sciences, especially those providing mechanistic insights into physiological functions at the molecular and cellular level, and clearly conveying a physiological message. Submissions are encouraged that deal with the evaluation of molecular and cellular mechanisms of disease, ideally resulting in translational research. Purely descriptive papers covering applied physiology or clinical papers will be excluded. Papers on methodological topics will be considered if they contribute to the development of novel tools for further investigation of (patho)physiological mechanisms.