ATP-citrate lyase (ACLY) in lipid metabolism and ... - PubMed
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 …
Liver-specific ATP-citrate lyase inhibition by bempedoic acid
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...
Bempedoic acid suppresses diet-induced hepatic steatosis
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.
Bempedoic acid suppresses diet-induced hepatic steatosis …
2024年10月28日 · 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.
Bempedoic Acid (ETC-1002): an Investigational Inhibitor of ATP Citrate ...
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 ...
Mechanism of action and therapeutic use of bempedoic acid in ...
First, bempedoic acid inhibits hepatic ATP-citrate lyase (ACLY), an enzyme that regulates the flow of extra-mitochondrial citrate in the synthesis of lipids. Second, it upregulates the AMP-activated protein kinase (AMPK), a pivotal kinase that controls energy homeostasis and inflammation at the whole organism level.
Liver-specific ATP-citrate lyase inhibition by bempedoic acid decreases ...
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.
Bempedoic Acid, the First-in-Class Oral ATP Citrate Lyase …
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 ...
Bempedoic Acid, the First-in-Class Oral ATP Citrate Lyase ... - MDPI
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 ...
Safety and Efficacy of Bempedoic Acid to Reduce LDL Cholesterol
2019年3月13日 · Bempedoic acid (8-hydroxy-2,2,14,14-tetramethylpentadecanedioic acid) is a small molecule that has been shown to lower the LDL cholesterol level by inhibiting ATP citrate lyase, a key enzyme in...