GPR146: an emerging therapeutic target for hypercholesterolemia and atherosclerosis  

作　　者：Lan She Hailun Yao Lingzhi He Yajun Li Jianping Cao 

机构地区：[1]Department of Medical College,Hunan Polytechnic of Environment and Biology,Hengyang 421001,China

出　　处：《Acta Biochimica et Biophysica Sinica》2020年第8期914-915,共2页生物化学与生物物理学报（英文版）

基　　金：This work was supported by the grant from the Pillar Project of Human Polytechnic of Environment and Biology(No.201933).

摘　　要：Recently, Yu et al. [1] revealed that G protein-coupled receptor 146 (GPR146) exerts a detrimental effect on the regulation of systemic cholesterol metabolism. Mechanically, GPR146 induces hepatic sterol regulatory element binding protein 2 (SREBP2) via the activation of extracellular signal-regulated kinase 1/2 (ERK1/2) signaling, consequently resulting in hepatic low-density lipoprotein (VLDL) secretion. Notably, GPR146 depletion reduces VLDL secretion and decreases aortic atherosclerotic lesions in low-density lipoprotein receptor (LDLR)-deficient mice via the suppression of ERK1/2/SREBP2 pathway, suggesting that GPR146 may contribute to the incidence of atherosclerosis (AS) and familial hypercholesterolemia (HoFH). Taken together, inhibition of GPR146 is likely to be an effective strategy for AS and HoFH treatment for modulating cholesterol levels.

关 键 词：GPR14 ATHEROSCLEROSIS CHOLESTEROL 

分 类 号：R97[医药卫生—药品]