ATP柠檬酸裂解酶
裂解酶
炎症
酶
生物
药理学
化学
生物化学
医学
柠檬酸合酶
免疫学
作者
Sanne G.S. Verberk,Kirsten L. Kuiper,Mario A. Lauterbach,Eicke Latz,Jan Van den Bossche
标识
DOI:10.1016/j.molmed.2021.09.004
摘要
ATP-citrate lyase (Acly) is the target of the new class low-density lipoprotein-cholesterol (LDL-C)-lowering drug bempedoic acid (BA). Acly is a key metabolic enzyme synthesizing acetyl-CoA as the building block of cholesterol and fatty acids. Treatment with BA lowers circulating lipid levels and reduces systemic inflammation, suggesting a dual benefit of this drug for atherosclerosis therapy. Recent studies have shown that targeting Acly in macrophages can attenuate inflammatory responses and decrease atherosclerotic plaque vulnerability. Therefore, it could be beneficial to extend the application of Acly inhibition from solely lipid-lowering by liver-specific inhibition to also targeting macrophages in atherosclerosis. Here, we outline the possibilities of targeting Acly and describe the future needs to translate these findings to the clinic.
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