Application | Comment | Organism |
---|---|---|
drug development | Mendelian randomization of large human cohorts has validated ACLY as a promising target for low-density-lipoprotein-cholesterol lowering and cardiovascular protection | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
bempedoic acid | i.e. ETC-1002 is a first-in-class, prodrug-based direct competitive inhibitor of ATP citrate lyase which regulates lipid metabolism by upregulating hepatic LDL receptor (LDLr) expression and activity. Pharmacological inhibition of ACLY by bempedoic acid, prevents dyslipidemia and attenuates atherosclerosis in hypercholesterolemic ApoE-/- mice, LDLr-/- mice, and LDLr-/- miniature pigs | Homo sapiens | |
SB-204990 | in addition to lowering lipids by inhibiting ACLY, the chemical inhibitor SB-204990 also displays tumor suppressive effects | Homo sapiens |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + citrate + CoA | Homo sapiens | ATP citrate lyase is an important enzyme linking carbohydrate to lipid metabolism by generating acetyl-CoA from citrate for fatty acid and cholesterol biosynthesis | ADP + phosphate + acetyl-CoA + oxaloacetate | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | P53396 | - |
- |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
hepatocyte | ACLY deficiency in hepatocytes protects from hepatic steatosis and dyslipidemia | Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + citrate + CoA | - |
Homo sapiens | ADP + phosphate + acetyl-CoA + oxaloacetate | - |
? | |
ATP + citrate + CoA | ATP citrate lyase is an important enzyme linking carbohydrate to lipid metabolism by generating acetyl-CoA from citrate for fatty acid and cholesterol biosynthesis | Homo sapiens | ADP + phosphate + acetyl-CoA + oxaloacetate | - |
? |
Synonyms | Comment | Organism |
---|---|---|
ACLY | - |
Homo sapiens |
ATP-citrate lyase | - |
Homo sapiens |
General Information | Comment | Organism |
---|---|---|
metabolism | ATP citrate lyase is an important enzyme linking carbohydrate to lipid metabolism by generating acetyl-CoA from citrate for fatty acid and cholesterol biosynthesis | Homo sapiens |