Yan Han, Liu Wenjun, Xiang Rui, Li Xin, Hou Song, Xu Luzheng, Wang Lin, Zhao Dong, Liu Xingkai, Wang Guoqing, Chi Yujing, Yang Jichun
Department of Physiology and Pathophysiology, School of Basic Medical Sciences, State Key Laboratory of Vascular Homeostasis and Remodeling, Center for Non-coding RNA Medicine, Peking University Health Science Center, Beijing, 100191, China.
Department of Endocrinology, The Second Affiliated Hospital, School of Medicine, Zhejiang University, Hangzhou, 310058, China.
Signal Transduct Target Ther. 2024 Aug 8;9(1):214. doi: 10.1038/s41392-024-01914-0.
Nonalcoholic fatty liver disease (NAFLD) is a serious threat to public health, but its underlying mechanism remains poorly understood. In screening important genes using Gene Importance Calculator (GIC) we developed previously, ribosomal modification protein rimK-like family member A (RIMKLA) was predicted as one essential gene but its functions remained largely unknown. The current study determined the roles of RIMKLA in regulating glucose and lipid metabolism. RIMKLA expression was reduced in livers of human and mouse with NAFLD. Hepatic RIMKLA overexpression ameliorated steatosis and hyperglycemia in obese mice. Hepatocyte-specific RIMKLA knockout aggravated high-fat diet (HFD)-induced dysregulated glucose/lipid metabolism in mice. Mechanistically, RIMKLA is a new protein kinase that phosphorylates betaine-homocysteine S-methyltransferase 1 (BHMT1) at threonine 45 (Thr45) site. Upon phosphorylation at Thr45 and activation, BHMT1 eliminated homocysteine (Hcy) to inhibit the activity of transcription factor activator protein 1 (AP1) and its induction on fatty acid synthase (FASn) and cluster of differentiation 36 (CD36) gene transcriptions, concurrently repressing lipid synthesis and uptake in hepatocytes. Thr45 to alanine (T45A) mutation inactivated BHMT1 to abolish RIMKLA's repression on Hcy level, AP1 activity, FASn/CD36 expressions, and lipid deposition. BHMT1 overexpression rescued the dysregulated lipid metabolism in RIMKLA-deficient hepatocytes. In summary, RIMKLA is a novel protein kinase that phosphorylates BHMT1 at Thr45 to repress lipid synthesis and uptake. Under obese condition, inhibition of RIMKLA impairs BHMT1 activity to promote hepatic lipid deposition.
非酒精性脂肪性肝病(NAFLD)对公众健康构成严重威胁,但其潜在机制仍知之甚少。在使用我们之前开发的基因重要性计算器(GIC)筛选重要基因时,核糖体修饰蛋白rimK样家族成员A(RIMKLA)被预测为一个关键基因,但其功能在很大程度上仍不清楚。当前的研究确定了RIMKLA在调节葡萄糖和脂质代谢中的作用。在患有NAFLD的人类和小鼠肝脏中,RIMKLA的表达降低。肝脏中RIMKLA的过表达改善了肥胖小鼠的脂肪变性和高血糖。肝细胞特异性RIMKLA基因敲除加重了高脂饮食(HFD)诱导的小鼠葡萄糖/脂质代谢失调。从机制上讲,RIMKLA是一种新的蛋白激酶,可在苏氨酸45(Thr45)位点磷酸化甜菜碱-同型半胱氨酸S-甲基转移酶1(BHMT1)。在Thr45位点磷酸化并激活后,BHMT1消除同型半胱氨酸(Hcy)以抑制转录因子激活蛋白1(AP1)的活性及其对脂肪酸合酶(FASn)和分化簇36(CD36)基因转录的诱导,同时抑制肝细胞中的脂质合成和摄取。Thr45突变为丙氨酸(T45A)使BHMT1失活,从而消除了RIMKLA对Hcy水平、AP1活性、FASn/CD36表达和脂质沉积的抑制作用。BHMT1的过表达挽救了RIMKLA缺陷型肝细胞中失调的脂质代谢。总之,RIMKLA是一种新型蛋白激酶,可在Thr45位点磷酸化BHMT1以抑制脂质合成和摄取。在肥胖条件下,抑制RIMKLA会损害BHMT1的活性,从而促进肝脏脂质沉积。