Tian Shasha, Zhou Saijun, Wu Weixi, Lin Yao, Wang Tongdan, Sun Haizhen, A-Ni-Wan A-Shan-Jiang, Li Yaru, Wang Chongyang, Li Xiaogang, Yu Pei, Zhao Yanjun
NHC Key Laboratory of Hormones and Development, Chu Hsien-I Memorial Hospital and Tianjin Institute of Endocrinology, Tianjin Key Laboratory of Metabolic Diseases, Tianjin Medical University, Tianjin, 300134, China.
Department of Nephrology, The Fifth Hospital of Shanxi Medical University (Shanxi Provincial People's Hospital), Taiyuan, Shanxi, 030000, China.
Adv Sci (Weinh). 2025 Jan;12(4):e2409781. doi: 10.1002/advs.202409781. Epub 2024 Dec 4.
Semaglutide (Smg), a GLP-1 receptor agonist (GLP-1RA), shows renal protective effects in patients with diabetic kidney disease (DKD). However, the exact underlying mechanism remains elusive. This study employs transcriptome sequencing and identifies β-Klotho (KLB) as the critical target responsible for the role of Smg in kidney protection. Smg treatment alleviates diabetic kidney injury by inhibiting ferroptosis in patients, animal models, and HK-2 cells. Notably, Smg treatment significantly increases the mRNA expression of KLB through the activation of the cyclic adenosine monophosphate (cAMP) signaling pathway, specifically through the phosphorylation of protein kinase A (PKA) and cAMP-response element-binding protein (CREB). Subsequently, the adenosine monophosphate-activated protein kinase (AMPK) signaling pathway is activated, reprograming the key metabolic processes of ferroptosis such as iron metabolism, fatty acid synthesis, and the antioxidant response against lipid peroxidation. Suppression of ferroptosis by Smg further attenuates renal inflammation and fibrosis. This work highlights the potential of GLP-1RAs and KLB targeting as promising therapeutic approaches for DKD management.
司美格鲁肽(Smg)是一种胰高血糖素样肽-1受体激动剂(GLP-1RA),对糖尿病肾病(DKD)患者具有肾脏保护作用。然而,确切的潜在机制仍不清楚。本研究采用转录组测序,确定β-klotho(KLB)是Smg发挥肾脏保护作用的关键靶点。在患者、动物模型和HK-2细胞中,Smg治疗通过抑制铁死亡减轻糖尿病肾损伤。值得注意的是,Smg治疗通过激活环磷酸腺苷(cAMP)信号通路,特别是通过蛋白激酶A(PKA)和cAMP反应元件结合蛋白(CREB)的磷酸化,显著增加KLB的mRNA表达。随后,腺苷单磷酸激活蛋白激酶(AMPK)信号通路被激活,重新编程铁死亡的关键代谢过程,如铁代谢、脂肪酸合成以及对脂质过氧化的抗氧化反应。Smg对铁死亡的抑制进一步减轻了肾脏炎症和纤维化。这项工作突出了GLP-1RAs和靶向KLB作为DKD治疗有前景的治疗方法的潜力。