ACL

ATP citrate lyase (ACL; EC 2.3.3. 8) is a cytosolic enzyme that catalyzes the synthesis of acetyl-CoA and oxaloacetate using citrate, CoA, and ATP as substrates and Mg2+ as a necessary cofactor, and it is expressed in lipogenic tissues such as liver and adipose[1]. In mammals, the formation of acetyl-CoA is an essential step for the de novo synthesis of fatty acid (FA) and cholesterol for converting the carbohydrate carbon energy source into lipids. Hence, it has been thought that ACL inhibition would be beneficial for the treatment of obesity and dyslipidemia through the simultaneous inhibition of endogenous synthesis of FA and cholesterol[2]. Interestingly, it was found that ACL is also required for increases in histone acetylation in response to growth factor stimulation and during differentiation, and that glucose availability can affect histone acetylation in an ACL-dependent manner[3].


[1] JJ Li et al. 2-hydroxy-N-arylbenzenesulfonamides as ATP-citrate lyase inhibitors. Bioorg Med Chem Lett. 2007 Jun 1;17(11):3208-11.
[2] Z Ma et al. A novel direct homogeneous assay for ATP citrate lyase. J Lipid Res. 2009 Oct;50(10):2131-5.
[3] KE Wellen et al. ATP-citrate lyase links cellular metabolism to histone acetylation. Science. 2009 May 22;324(5930):1076-80.

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Axon ID Name Description From price
2506 BMS 303141 Cell-permeable ATP-citrate lyase (ACL) inhibitor €90.00

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