2016年11月28日 · Bempedoic acid (ETC-1002) is a small molecule intended to lower LDL-C in hypercholesterolemic patients, and has been previously shown to modulate both ATP-citrate lyase (ACL) and AMP-activated protein kinase (AMPK) activity in rodents.

ATP citrate lyase (ACLY) is an important enzyme linking carbohydrate to lipid metabolism by generating acetyl-CoA from citrate for fatty acid and cholesterol biosynthesis. Mendelian randomization of large human cohorts has validated ACLY as a promising target for low-density-lipoprotein-cholesterol …

2024年11月23日 · 近日，宾夕法尼亚大学Kathryn E. Wellen实验室等在Cell Metabolism杂志发表了Bempedoic acid suppresses diet-induced hepatic steatosis independently of ATP-citrate lyase研究文章，探讨了BPA在肝脏脂质代谢中的作用机制，发现BPA通过独立于ATP-柠檬酸裂解酶（ACLY）的途径抑制饮食诱导的肝 ...

2021年9月4日 · Bempedoic acid (ETC-1002), a ATP citrate lyase (ACLY) inhibitor that lowers the LDL cholesterol was recently approved by US FDA for the treatment of heterozygous familial hypercholesterolemia (HeFH) and established atherosclerotic cardiovascular disease (ASCVD).

2016年11月28日 · ATP-citrate lyase (ACL) is a cytosolic enzyme upstream of HMG-CoA reductase in the lipid biosynthesis pathway that catalyses the cleavage of mitochondrial-derived citrate into oxaloacetate...

Bempedoic acid (ETC-1002) is one such novel cholesterol-lowering drug. It is an inhibitor of adenosine triphosphate (ATP) citrate lyase (ACL), a cellular enzyme responsible for production of precursors for fatty acid and cholesterol synthesis. ETC-1002 effectively reduces LDL-C and apolipoprotein (apo) B–containing lipoproteins [11••]. In ...

2024年10月26日 · Bempedoic acid–CoA is a potent and selective inhibitor of ATP citrate lyase (ACL), a key enzyme in the biosynthetic pathway of cholesterol and fatty acids. The drug reduces low-density lipoprotein–cholesterol (LDL-C) (20–25%), non-high-density lipoprotein–cholesterol (HDL-C) (19%), apolipoprotein B (apoB) (15%), and total cholesterol ...

ATP citrate lyase (ACLY) synthesizes acetyl-CoA for de novo lipogenesis (DNL), which is elevated in metabolic dysfunction-associated steatotic liver disease. Hepatic ACLY is inhibited by the LDL-cholesterol-lowering drug bempedoic acid (BPA), which also improves steatosis in mice.

ATP-citrate lyase (ACL) is a cytosolic enzyme upstream of HMG-CoA reductase in the lipid biosynthesis pathway that catalyses the cleavage of mitochondrial-derived citrate into oxaloacetate and acetyl-CoA, the latter serving as common substrate for de novo cholesterol and fatty acid synthesis.

Bempedoic acid is a new cholesterol-lowering drug, which has recently received US FDA and EMA approval. This drug targets lipid and glucose metabolism as well as inflammation via downregulation of ATP-citrate lyase and upregulation of AMP-activated protein kinase (AMPK).