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Characterization of ATP citrate lyase from Chlorobium limicola

Journal of Bacteriology, 1982
ATP citrate lyase (EC 4.1.3.8) from Chlorobium limicola was partially purified. It was established that the consumption of substrates and the formation of products proceeded stoichiometrically and that citrate cleavage was of the si-type. ADP and oxaloacetate inhibited enzyme activity. Oxaloacetate also inhibited the growth of C. limicola.
G, Antranikian   +2 more
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Binding of hydroxycitrate to human ATP-citrate lyase

Acta Crystallographica Section D Structural Biology, 2017
Hydroxycitrate from the fruit ofGarcinia cambogia[i.e.(2S,3S)-2-hydroxycitrate] is the best-known inhibitor of ATP-citrate lyase. Well diffracting crystals showing how the inhibitor binds to human ATP-citrate lyase were grown by modifying the protein. The protein was modified by introducing cleavage sites forTobacco etch virusprotease on either side of
Jinhong, Hu   +2 more
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Discovery of a Novel Macrocyclic ATP Citrate Lyase Inhibitor

Journal of Chemical Information and Modeling, 2022
ATP citrate lyase (ACLY) is an important metabolic enzyme involved in the synthesis of fatty acid and cholesterol. The inhibition of ACLY is considered as a promising therapeutic strategy for various metabolic diseases and numerous malignancies. In this study, a novel macrocyclic compound 2 has been identified as a potent ACLY inhibitor with the "ring ...
Yongjun Zang   +7 more
openaire   +2 more sources

On the Catalytic Mechanism of Human ATP Citrate Lyase

Biochemistry, 2012
ATP citrate lyase (ACL) catalyzes an ATP-dependent biosynthetic reaction which produces acetyl-coenzyme A and oxaloacetate from citrate and coenzyme A (CoA). Studies were performed with recombinant human ACL to ascertain the nature of the catalytic phosphorylation that initiates the ACL reaction and the identity of the active site residues involved ...
Fan, Fan   +9 more
openaire   +2 more sources

ATP Citrate Lyase Inhibitors as Novel Cancer Therapeutic Agents

Recent Patents on Anti-Cancer Drug Discovery, 2012
ATP citrate lyase (ACL or ACLY) is an extra-mitochondrial enzyme widely distributed in various human and animal tissues. ACL links glucose and lipid metabolism by catalyzing the formation of acetyl-CoA and oxaloacetate from citrate produced by glycolysis in the presence of ATP and CoA.
Xu-Yu, Zu   +7 more
openaire   +2 more sources

2-Hydroxy-N-arylbenzenesulfonamides as ATP-citrate lyase inhibitors

Bioorganic & Medicinal Chemistry Letters, 2007
A novel series of 2-hydroxy-N-arylbenzenesulfonamides were identified to be ATP-citrate lyase (ACL) inhibitors with compound 9 displaying potent in vitro activity (IC(50)=0.13 microM). Chronic oral dosing of compound 9 in high-fat fed mice lowered plasma cholesterol, triglyceride, and glucose, as well as inhibited weight gain.
James J, Li   +20 more
openaire   +2 more sources

Targeting ATP-Citrate Lyase in Hyperlipidemia and Metabolic Disorders

Trends in Molecular Medicine, 2017
Chronic overnutrition and a sedentary lifestyle promote imbalances in metabolism, often manifesting as risk factors for life-threating diseases such as atherosclerotic cardiovascular disease (ASCVD) and nonalcoholic fatty liver disease (NAFLD). Nucleocytosolic acetyl-coenzyme A (CoA) has emerged as a central signaling node used to coordinate metabolic ...
Stephen L, Pinkosky   +3 more
openaire   +2 more sources

Discovery of Allosteric Inhibition of Human ATP-Citrate Lyase

Trends in Pharmacological Sciences, 2019
ATP-citrate lyase (ACLY) is an enzyme that links glycolysis to lipid metabolism. To date only partial X-ray structures of ACLY have been solved, thus limiting the design of novel inhibitors. Wei and colleagues (published online in Nature April 3, 2019) now report the full structure of human ACLY in complex with NDI-091143, revealing an appealing ...
openaire   +3 more sources

Role of ATP in the ATP citrate lyase reaction

Biochemical and Biophysical Research Communications, 1967
H, Inoue   +3 more
openaire   +2 more sources

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