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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

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

Inhibition of ATP-citrate lyase improves NASH, liver fibrosis, and dyslipidemia

Cell Metabolism, 2022
Battsetseg Batchuluun   +2 more
exaly  

ATP-citrate lyase (ACLY) inhibitors as therapeutic agents: a patenting perspective

Expert Opinion on Therapeutic Patents, 2022
Carlotta Granchi
exaly  

ATP citrate (pro-3S)-lyase

1990
Dietmar Schomburg, Margit Salzmann
openaire   +1 more source

ATP-citrate lyase (ACLY) in lipid metabolism and atherosclerosis: An updated review

Progress in Lipid Research, 2020
Xiaojun Feng, Suo-wen Xu, Ai-Zong Shen
exaly  

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