ATP-citrate lyase: genetics, molecular biology and therapeutic target for dyslipidemia

Ezetimibe Added to Statin Therapy after Acute Coronary Syndromes

Cannon, C. P., Blazing, M. A., Giugliano, R. P., McCagg, A., White, J. A., Theroux, P., Darius, H., Lewis, B. S., Ophuis, T. O., Jukema, J. W., et al. (2015) · New England Journal of Medicine · doi:10.1056/nejmoa1410489 · Cited by 4,487 · see citing works

ATP-citrate lyase links cellular metabolism to histone acetylation

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AMPK in Health and Disease

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ATP citrate lyase inhibition can suppress tumor cell growth

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Increased de novo lipogenesis is a distinct characteristic of individuals with nonalcoholic fatty liver disease

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Cholesterol Lowering in Intermediate-Risk Persons without Cardiovascular Disease

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Association of LDL Cholesterol, Non–HDL Cholesterol, and Apolipoprotein B Levels With Risk of Cardiovascular Events Among Patients Treated With Statins: A Meta-analysis

Boekholdt, S. M., Arsenault, B. J., Mora, S., Pedersen, T. R., LaRosa, J. C., Nestel, P. J., Simes, R. J., Durrington, P., Hitman, G. A., Welch, K. M. A., et al. (2012) · JAMA · doi:10.1001/jama.2012.366 · Cited by 795 · see citing works

A meta-analysis of low-density lipoprotein cholesterol, non-high-density lipoprotein cholesterol, and apolipoprotein B as markers of cardiovascular risk

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ATP-Citrate Lyase: A Key Player in Cancer Metabolism

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ATP citrate lyase is an important component of cell growth and transformation

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Liver-specific ATP-citrate lyase inhibition by bempedoic acid decreases LDL-C and attenuates atherosclerosis

Pinkosky, S. L., Newton, R. S., Day, E. A., Ford, R. J., Lhotak, S., Austin, R. C., Birch, C. M., Smith, B. K., Filippov, S., Groot, P. H. E., et al. (2016) · Nature Communications · doi:10.1038/ncomms13457 · Cited by 498 · see citing works

ATP citrate lyase: activation and therapeutic implications in non-small cell lung cancer

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ATP-citrate lyase controls a glucose-to-acetate metabolic switch

Zhao, S., Torres, A., Henry, R. A., Trefely, S., Wallace, M., Lee, J. V., Carrer, A., Sengupta, A., Campbell, S. L., Kuo, Y.-M., et al. (2016) · Cell Reports · doi:10.1016/j.celrep.2016.09.069 · Cited by 394 · see citing works

Tricarballylate and hydroxycitrate: Substrate and inhibitor of ATP: Citrate oxaloacetate lyase

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ATP-citrate lyase: A mini-review

Chypre, M., Zaidi, N., & Smans, K. A. (2012) · Biochemical and Biophysical Research Communications · doi:10.1016/j.bbrc.2012.04.144 · Cited by 250 · see citing works

AMP-activated protein kinase and ATP-citrate lyase are two distinct molecular targets for ETC-1002, a novel small molecule regulator of lipid and carbohydrate metabolism

Pinkosky, S. L., Filippov, S. I., Srivastava, R. A. K., Hanselman, J. C., Bradshaw, C. D., Hurley, T. R., Cramer, C. T., Spahr, M. A., Brant, A. F., Houghton, J. L., et al. (2012) · Journal of Lipid Research · doi:10.1194/jlr.m030528 · Cited by 240 · see citing works

Abrogation of hepatic ATP-citrate lyase protects against fatty liver and ameliorates hyperglycemia in leptin receptor-deficient mice #

Wang, Q. A., Jiang, L., Wang, J., Li, S., Yu, Y., You, J., Zeng, R., Gao, X., Rui, L., Li, W., et al. (2008) · Hepatology · doi:10.1002/hep.22774 · Cited by 212 · see citing works

Phosphorylation of ATP-Citrate Lyase by Nucleoside Diphosphate Kinase

Wagner, P. D., & Vu, N. (1995) · Journal of Biological Chemistry · doi:10.1074/jbc.270.37.21758 · Cited by 195 · see citing works

Phosphorylation of Recombinant Human ATP:Citrate Lyase by cAMP-Dependent Protein Kinase Abolishes Homotropic Allosteric Regulation of the Enzyme by Citrate and Increases the Enzyme Activity. Allosteric Activation of ATP:Citrate Lyase by Phosphorylated Sugars

Potapova, I. A., El‐Maghrabi, M. R., Doronin, S. V., & Benjamin, W. B. (2000) · Biochemistry · doi:10.1021/bi992159y · Cited by 177 · see citing works

Efficacy and Safety of a Novel Dual Modulator of Adenosine Triphosphate-Citrate Lyase and Adenosine Monophosphate-Activated Protein Kinase in Patients With Hypercholesterolemia

Ballantyne, C. M., Davidson, M. H., MacDougall, D. E., Bays, H. E., DiCarlo, L. A., Rosenberg, N. L., Margulies, J., & Newton, R. S. (2013) · Journal of the American College of Cardiology · doi:10.1016/j.jacc.2013.05.050 · Cited by 175 · see citing works

AMPK β1 Deletion Reduces Appetite, Preventing Obesity and Hepatic Insulin Resistance

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Efficacy and Safety of ETC-1002, a Novel Investigational Low-Density Lipoprotein-Cholesterol–Lowering Therapy for the Treatment of Patients With Hypercholesterolemia and Type 2 Diabetes Mellitus

Gutierrez, M. J., Rosenberg, N. L., MacDougall, D. E., Hanselman, J. C., Margulies, J. R., Strange, P., Milad, M. A., McBride, S. J., & Newton, R. S. (2014) · Arteriosclerosis Thrombosis and Vascular Biology · doi:10.1161/atvbaha.113.302677 · Cited by 170 · see citing works

Efficacy and Safety of Rosuvastatin Therapy for Children With Familial Hypercholesterolemia

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The Lipogenesis Pathway as a Cancer Target

Abramson, H. N. (2011) · Journal of Medicinal Chemistry · doi:10.1021/jm2005805 · Cited by 166 · see citing works

A Role for ATP-Citrate Lyase, Malic Enzyme, and Pyruvate/Citrate Cycling in Glucose-induced Insulin Secretion

Guay, C., Madiraju, S. R. M., Aumais, A., Joly, E. C., & Prentki, M. (2007) · Journal of Biological Chemistry · doi:10.1074/jbc.m707294200 · Cited by 158 · see citing works

Use of ETC-1002 to treat hypercholesterolemia in patients with statin intolerance

Thompson, P. D., Rubino, J., Janik, M. J., MacDougall, D. E., McBride, S. J., Margulies, J. R., & Newton, R. S. (2015) · Journal of clinical lipidology · doi:10.1016/j.jacl.2015.03.003 · Cited by 158 · see citing works

ATP-Citrate Lyase Deficiency in the Mouse

Beigneux, A. P., Kosinski, C., Gavino, B. J., Horton, J. D., Skarnes, W. C., & Young, S. G. (2004) · Journal of Biological Chemistry · doi:10.1074/jbc.m310512200 · Cited by 154 · see citing works

Identification of ATP citrate lyase as a phosphoprotein.

Linn, T. C., & Srere, P. A. (1979) · Journal of Biological Chemistry · doi:10.1016/s0021-9258(17)37828-6 · Cited by 147 · see citing works

The role of ATP citrate-lyase in the metabolic regulation of plasma lipids

PEARCE, N. J., Yates, J. W., Berkhout, T. A., Jackson, B., Tew, D. G., Boyd, H., Camilleri, P., Sweeney, P. J., Gribble, A. D., Shaw, A. N., et al. (1998) · Biochemical Journal · doi:10.1042/bj3340113 · Cited by 144 · see citing works

Transcriptional Regulation of the ATP Citrate-lyase Gene by Sterol Regulatory Element-binding Proteins

Sato, R., Okamoto, A., Inoue, J., Miyamoto, W., Sakai, Y., Emoto, N., Shimano, H., & Maeda, M. (2000) · Journal of Biological Chemistry · doi:10.1074/jbc.275.17.12497 · Cited by 142 · see citing works

Treatment with ETC-1002 alone and in combination with ezetimibe lowers LDL cholesterol in hypercholesterolemic patients with or without statin intolerance

Thompson, P. D., MacDougall, D. E., Newton, R. S., Margulies, J. R., Hanselman, J. C., Orloff, D. G., McKenney, J. M., & Ballantyne, C. M. (2016) · Journal of clinical lipidology · doi:10.1016/j.jacl.2015.12.025 · Cited by 142 · see citing works

Rat ATP citrate-lyase. Molecular cloning and sequence analysis of a full-length cDNA and mRNA abundance as a function of diet, organ, and age.

Elshourbagy, N. A., Near, J. C., Kmetz, P., Sathe, G. M., Southan, C., Strickler, J. E., Gross, M. S., Young, J. F., Wells, T. N. C., & Groot, P. H. E. (1990) · Journal of Biological Chemistry · doi:10.1016/s0021-9258(19)40033-1 · Cited by 130 · see citing works

Bempedoic Acid (ETC-1002): an Investigational Inhibitor of ATP Citrate Lyase

Bilen, O., & Ballantyne, C. M. (2016) · Current Atherosclerosis Reports · doi:10.1007/s11883-016-0611-4 · Cited by 119 · see citing works

Decreased levels of metabolic enzymes in pancreatic islets of patients with type 2 diabetes

MacDonald, M. J., Longacre, M. J., Langberg, E.-C., Tibell, A., Kendrick, M. A., Fukao, T., & Ostenson, C.-G. (2009) · Diabetologia · doi:10.1007/s00125-009-1319-6 · Cited by 115 · see citing works

Statin myotoxicity: a review of genetic susceptibility factors

Needham, M., & Mastaglia, F. L. (2014) · Neuromuscular Disorders · doi:10.1016/j.nmd.2013.09.011 · Cited by 108 · see citing works

ATP citrate lyase knockdown impacts cancer stem cells in vitro

Hanai, J.-I., Doro, N. C., Seth, P., & Sukhatme, V. P. (2013) · Cell Death and Disease · doi:10.1038/cddis.2013.215 · Cited by 99 · see citing works

ETC-1002 regulates immune response, leukocyte homing, and adipose tissue inflammation via LKB1-dependent activation of macrophage AMPK

Filippov, S. I., Pinkosky, S. L., Lister, R. J., Pawloski, C., Hanselman, J. C., Cramer, C. T., Srivastava, R. A. K., Hurley, T. R., Bradshaw, C. D., Spahr, M. A., et al. (2013) · Journal of Lipid Research · doi:10.1194/jlr.m035212 · Cited by 90 · see citing works

Cloning and expression of a human ATP‐citrate lyase cDNA

Elshourbagy, N. A., Near, J. C., Kmetz, P., Wells, T. N. C., Groot, P. H. E., SAXTY, B. A., HUGHES, S. A., FRANKLIN, M., & Gloger, I. (1992) · European Journal of Biochemistry · doi:10.1111/j.1432-1033.1992.tb16659.x · Cited by 83 · see citing works

Effects of a novel dual lipid synthesis inhibitor and its potential utility in treating dyslipidemia and metabolic syndrome

Cramer, C. T., Goetz, B. D., Hopson, K. L., Fici, G. J., Ackermann, R., Brown, S. C., Bisgaier, C. L., Rajeswaran, W. G., Oniciu, D. C., & Pape, M. E. (2004) · Journal of Lipid Research · doi:10.1194/jlr.m400018-jlr200 · Cited by 74 · see citing works

Deficiency in hepatic ATP-citrate lyase affects VLDL-triglyceride mobilization and liver fatty acid composition in mice

Wang, Q. A., Li, S., Jiang, L., Zhou, Y., Li, Z., Shao, M., Li, W., & Liu, Y. (2010) · Journal of Lipid Research · doi:10.1194/jlr.m003335 · Cited by 68 · see citing works

ATP-Citrate Lyase Reduction Mediates Palmitate-induced Apoptosis in Pancreatic Beta Cells

Chu, K. Y., Lin, Y., Hendel, A., Kulpa, J. E., Brownsey, R. W., & Johnson, J. D. (2010) · Journal of Biological Chemistry · doi:10.1074/jbc.m110.157172 · Cited by 67 · see citing works

ATP ‐citrate lyase regulates cellular senescence via an AMPK ‐ and p53‐dependent pathway

Lee, J., Jang, H., Lee, S., Lee, J., Choi, J., Kim, T. W., Cho, E., & Youn, H. (2014) · FEBS Journal · doi:10.1111/febs.13139 · Cited by 62 · see citing works

Effects of nutrients and hormones on gene expression of ATP citrate‐lyase in rat liver

Fukuda, H., Katsurada, A., & Iritani, N. (1992) · European Journal of Biochemistry · doi:10.1111/j.1432-1033.1992.tb17279.x · Cited by 51 · see citing works

Adenosine triphosphate citrate lyase: Emerging target in the treatment of dyslipidemia

Lemus, H. N., & Mendivil, C. O. (2015) · Journal of clinical lipidology · doi:10.1016/j.jacl.2015.01.002 · Cited by 49 · see citing works

Polymorphisms, de novo lipogenesis, and plasma triglyceride response following fish oil supplementation

Bouchard‐Mercier, A., Rudkowska, I., Lemieux, S., Couture, P., & Vohl, M. (2013) · Journal of Lipid Research · doi:10.1194/jlr.m041590 · Cited by 25 · see citing works

ADP–Mg2+bound to the ATP-grasp domain of ATP-citrate lyase

Sun, T., Hayakawa, K., & Fraser, M. E. (2011) · Acta Crystallographica Section F Structural Biology and Crystallization Communications · doi:10.1107/s1744309111028363 · Cited by 22 · see citing works

Genome-wide pathway analysis in attention-deficit/hyperactivity disorder

Lee, Y. H., & Song, G. G. (2014) · Neurological Sciences · doi:10.1007/s10072-014-1671-2 · Cited by 19 · see citing works

Fatty Acid Synthesis Pathway Genetic Variants and Clinical Outcome of Non-Small Cell Lung Cancer Patients after Surgery

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Binding of ATP citrate lyase to the microsomal fraction of rat liver.

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Functional polymorphisms of ATP citrate lyase gene predicts clinical outcome of patients with advanced colorectal cancer

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Influence of Various Central Moieties on the Hypolipidemic Properties of Long Hydrocarbon Chain Diols and Diacids

Oniciu, D. C., Dasseux, J., Yang, J., Mueller, R., Pop, E., Denysenko, A., Duan, C., Huang, T., Zhang, L., Krause, B. R., et al. (2005) · Journal of Medicinal Chemistry · doi:10.1021/jm050650j · Cited by 12 · see citing works

Polymorphisms in Genes of the De Novo Lipogenesis Pathway and Overall Survival of Hepatocellular Carcinoma Patients Undergoing Transarterial Chemoembolization

Wu, Y., Bao, D., Dai, J., Chen, C. Y., Zhang, H., Yang, Y., Xing, J., Huang, X., & Wan, S.-G. (2015) · Asian Pacific Journal of Cancer Prevention · doi:10.7314/apjcp.2015.16.3.1051 · Cited by 11 · see citing works

Abstract 17499: ETC-1002 Incrementally Lowers Low Density Lipoprotein-cholesterol in Patients With Hypercholesterolemia Receiving Stable Statin Therapy

Ballantyne, C. M., MacDougall, D. E., Margulies, J. R., Robinson, P. L., Hanselman, J. C., & Lalwani, N. D. (2015) · Circulation · doi:10.1161/circ.132.suppl_3.17499 · Cited by 4 · see citing works

Abstract 18: Bempedoic Acid Lowers Low Density Lipoprotein-Cholesterol and Attenuates Aortic Atherosclerosis in LDL Receptor-Deficient ( LDLR +/- and LDLR -/- ) Yucatan Miniature Pigs

Burke, A. C., Telford, D. E., Sutherland, B. G., Edwards, J. Y., Sawyez, C. G., Newton, R. S., & Huff, M. W. (2016) · Arteriosclerosis Thrombosis and Vascular Biology · doi:10.1161/atvb.36.suppl_1.18 · Cited by 1 · see citing works

Lipid-droplet-accumulating microglia represent a dysfunctional and proinflammatory state in the aging brain

Marschallinger, J., Iram, T., Zardeneta, M., Lee, S. E., Lehallier, B., Haney, M. S., Pluvinage, J. V., Mathur, V., Hahn, O., Morgens, D. W., et al. (2020) · Nature Neuroscience · doi:10.1038/s41593-019-0566-1 · Cited by 1,384 · see citing works

Acetyl-CoA metabolism in cancer

Guertin, D. A., & Wellen, K. E. (2023) · Nature Reviews Cancer · doi:10.1038/s41568-022-00543-5 · Cited by 303 · see citing works

Lipid management in patients with chronic kidney disease

Ferro, C. J., Mark, P. B., Kanbay, M., Sarafidis, P. A., Heine, G. H., Rossignol, P., Massy, Z. A., Mallamaci, F., Valdivielso, J. M., Małyszko, J., et al. (2018) · Nature Reviews Nephrology · doi:10.1038/s41581-018-0072-9 · Cited by 275 · see citing works

ATP citrate lyase: A central metabolic enzyme in cancer

Icard, P., Wu, Z., Fournel, L., Coquerel, A., Lincet, H., & Alifano, M. (2019) · Cancer Letters · doi:10.1016/j.canlet.2019.12.010 · Cited by 240 · see citing works

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

Feng, X., Zhang, L., Xu, S., & Shen, A.-Z. (2019) · Progress in Lipid Research · doi:10.1016/j.plipres.2019.101006 · Cited by 233 · see citing works

Acetyl-CoA Metabolism and Histone Acetylation in the Regulation of Aging and Lifespan

Bradshaw, P. C. (2021) · Antioxidants · doi:10.3390/antiox10040572 · Cited by 185 · see citing works

Metabolic landscape in cardiac aging: insights into molecular biology and therapeutic implications

Xie, S., Xu, S., Deng, W., & Tang, Q. (2023) · Signal Transduction and Targeted Therapy · doi:10.1038/s41392-023-01378-8 · Cited by 185 · see citing works

An allosteric mechanism for potent inhibition of human ATP-citrate lyase

Jia, W., Leit, S. M., Kuai, J., Therrien, É., Rafi, S. B., Harwood, H. J., DeLaBarre, B., & Tong, L. (2019) · Nature · doi:10.1038/s41586-019-1094-6 · Cited by 184 · see citing works

Lipid-Lowering Agents: Targets Beyond PCSK9

Hegele, R. A., & Tsimikas, S. (2019) · Circulation Research · doi:10.1161/circresaha.118.313171 · Cited by 171 · see citing works

The IKKβ‐USP30‐ACLY Axis Controls Lipogenesis and Tumorigenesis

Gu, L., Zhu, Y., Lin, X., Lu, B., Zhou, X., Zhou, F., Zhao, Q., Prochownik, E. V., & Li, Y. (2020) · Hepatology · doi:10.1002/hep.31249 · Cited by 147 · see citing works

Molecular Regulation of Lipogenesis, Adipogenesis and Fat Deposition in Chicken

Nematbakhsh, S., Chong, P. P., Selamat, J., Nordin, N., Idris, L. H., & Razis, A. F. A. (2021) · Genes · doi:10.3390/genes12030414 · Cited by 139 · see citing works

Macrophage ATP citrate lyase deficiency stabilizes atherosclerotic plaques

Baardman, J., Verberk, S. G. S., van der Velden, S., Gijbels, M. J., van Roomen, C. P. A. A., Sluimer, J. C., Broos, J. Y., Griffith, G. R., Prange, K. H. M., van Weeghel, M., et al. (2020) · Nature Communications · doi:10.1038/s41467-020-20141-z · Cited by 127 · see citing works

Key Molecules of Fatty Acid Metabolism in Gastric Cancer

Li, C., Zhang, L., Qiu, Z., Deng, W., & Wang, W. (2022) · Biomolecules · doi:10.3390/biom12050706 · Cited by 113 · see citing works

Prevention of Diet-Induced Metabolic Dysregulation, Inflammation, and Atherosclerosis in Ldlr −/− Mice by Treatment With the ATP-Citrate Lyase Inhibitor Bempedoic Acid

Samsoondar, J. P., Burke, A. C., Sutherland, B. G., Telford, D. E., Sawyez, C. G., Edwards, J. Y., Pinkosky, S. L., Newton, R. S., & Huff, M. W. (2017) · Arteriosclerosis Thrombosis and Vascular Biology · doi:10.1161/atvbaha.116.308963 · Cited by 96 · see citing works

Cryo-EM as a powerful tool for drug discovery

Drie, J. H. V., & Tong, L. (2020) · Bioorganic & Medicinal Chemistry Letters · doi:10.1016/j.bmcl.2020.127524 · Cited by 94 · see citing works

Dyslipidemia Management in Adults With Diabetes

Lazarte, J., & Hegele, R. A. (2019) · Canadian Journal of Diabetes · doi:10.1016/j.jcjd.2019.07.003 · Cited by 87 · see citing works

The vital role of ATP citrate lyase in chronic diseases

Khwairakpam, A. D., Banik, K., Girisa, S., Shabnam, B., Shakibaei, M., Fan, L., Arfuso, F., Monisha, J., Wang, H., Mao, X., et al. (2019) · Journal of Molecular Medicine · doi:10.1007/s00109-019-01863-0 · Cited by 87 · see citing works

Effects of Food Additives on Immune Cells As Contributors to Body Weight Gain and Immune-Mediated Metabolic Dysregulation

Neto, H. A. P., Ausina, P., Gomez, L. S., Leandro, J. G. B., Zancan, P., & Sola‐Penna, M. (2017) · Frontiers in Immunology · doi:10.3389/fimmu.2017.01478 · Cited by 77 · see citing works

Parental metabolic syndrome epigenetically reprograms offspring hepatic lipid metabolism in mice

Jesus, D. F. D., Orime, K., Kamińska, D., Kimura, T., Basile, G., Wang, C., Haertle, L., Riemens, R. J. M., Brown, N. K., Hu, J., et al. (2020) · Journal of Clinical Investigation · doi:10.1172/jci127502 · Cited by 68 · see citing works

Research progress on the pharmacological effects of berberine targeting mitochondria

Fang, X., Wu, H., Wei, J., Miao, R., Zhang, Y., & Tian, J. (2022) · Frontiers in Endocrinology · doi:10.3389/fendo.2022.982145 · Cited by 72 · see citing works

Molecular basis for acetyl-CoA production by ATP-citrate lyase

Wei, X., Schultz, K. C., Bazilevsky, G. A., Vogt, A. D., & Marmorstein, R. (2019) · Nature Structural & Molecular Biology · doi:10.1038/s41594-019-0351-6 · Cited by 58 · see citing works

An integrative multiomic network model links lipid metabolism to glucose regulation in coronary artery disease

Cohain, A. T., Barrington, W. T., Jordan, D. M., Beckmann, N. D., Argmann, C., Houten, S. M., Charney, A. W., Ermel, R., Sukhavasi, K., Franzén, O., et al. (2021) · Nature Communications · doi:10.1038/s41467-020-20750-8 · Cited by 58 · see citing works

ETC-1002 (Bempedoic acid) for the management of hyperlipidemia: from preclinical studies to phase 3 trials

Ruscica, M., Banach, M., Sahebkar, A., Corsini, A., & Sirtori, C. R. (2019) · Expert Opinion on Pharmacotherapy · doi:10.1080/14656566.2019.1583209 · Cited by 55 · see citing works

Salidroside simultaneously reduces de novo lipogenesis and cholesterol biosynthesis to attenuate atherosclerosis in mice

Song, T., Wang, P., Li, C., Li, J. X., Liang, Q., Cao, Y., Dong, P., Shi, H., & Jiang, M. (2020) · Biomedicine & Pharmacotherapy · doi:10.1016/j.biopha.2020.111137 · Cited by 52 · see citing works

USP30: Structure, Emerging Physiological Role, and Target Inhibition

Wang, F., Gao, Y. P., Zhou, L., Chen, J., Xie, Z., Ye, Z., & Wang, Y. (2022) · Frontiers in Pharmacology · doi:10.3389/fphar.2022.851654 · Cited by 51 · see citing works

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

Granchi, C. (2022) · Expert Opinion on Therapeutic Patents · doi:10.1080/13543776.2022.2067478 · Cited by 47 · see citing works

Lipid droplets in central nervous system and functional profiles of brain cells containing lipid droplets in various diseases

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Bempedoic Acid Lowers Low-Density Lipoprotein Cholesterol and Attenuates Atherosclerosis in Low-Density Lipoprotein Receptor–Deficient ( LDLR +/− and LDLR −/− ) Yucatan Miniature Pigs

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Fatty acid metabolism-related enzymes in colorectal cancer metastasis: from biological function to molecular mechanism

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Lipid lowering drugs and inflammatory changes: an impact on cardiovascular outcomes?

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Phytochemical and biological studies on rare and endangered plants endemic to China. Part XV. Structurally diverse diterpenoids and sesquiterpenoids from the vulnerable conifer

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Nuclear localization of metabolic enzymes in immunity and metastasis

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Targeting metabolic reprogramming in hepatocellular carcinoma to overcome therapeutic resistance: A comprehensive review

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Bempedoic Acid (ETC-1002): ATP Citrate Lyase Inhibitor

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ACLY inhibitors induce apoptosis and potentiate cytotoxic effects of sorafenib in thyroid cancer cells

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Adenosine Triphosphate Citrate Lyase and Fatty Acid Synthesis Inhibition

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Identification of key genes involved in type 2 diabetic islet dysfunction: a bioinformatics study

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Modulation of matrix metabolism by ATP-citrate lyase in articular chondrocytes

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ATP-citrate lyase multimerization is required for coenzyme-A substrate binding and catalysis

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Structure of ACLY in complex with CoA

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Emerging lipid lowering agents targeting LDL cholesterol

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Emerging Fixed-Dose Combination Treatments for Hyperlipidemia

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Bempedoic acid, an ATP citrate lyase inhibitor, reduces intimal hyperplasia via activation of AMPKα signaling pathway

Liu, W., Liu, M., Xiong, H., Xia, L., Yang, Q., Chen, M., Cai, Y., & Li, S. (2022) · International Immunopharmacology · doi:10.1016/j.intimp.2022.109392 · Cited by 22 · see citing works

Human adipocyte differentiation and composition of disease-relevant lipids are regulated by miR-221-3p

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D-2-hydroxyglutarate dehydrogenase governs adult neural stem cell activation and promotes histone acetylation via ATP-citrate lyase

Liu, Y., Wang, M., Guo, Y., Wang, L., & Guo, W. (2023) · Cell Reports · doi:10.1016/j.celrep.2023.112067 · Cited by 20 · see citing works

Mice exposed to maternal androgen excess and diet-induced obesity have altered phosphorylation of catechol-O-methyltransferase in the placenta and fetal liver

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Therapeutic Agents Targeting Cardiometabolic Risk for Preventing and Treating Atherosclerotic Cardiovascular Diseases

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Crosstalk of hepatocyte nuclear factor 4a and glucocorticoid receptor in the regulation of lipid metabolism in mice fed a high-fat-high-sugar diet

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Comparing Transcriptomes Reveals Key Metabolic Mechanisms in Superior Growth Performance Nile Tilapia (Oreochromis niloticus)

Chen, B., Xiao, W., Zou, Z., Zhu, J., Li, D., Yu, J., & Yang, H. (2022) · Frontiers in Genetics · doi:10.3389/fgene.2022.879570 · Cited by 18 · see citing works

A role for ATP Citrate Lyase in cell cycle regulation during myeloid differentiation

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Bempedoic Acid and Ezetimibe for the Treatment of Hypercholesterolemia: A Systematic Review and Meta-Analysis of Randomized Phase II/III trials

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Unprecedented spirodioxynaphthalenes from the endophytic fungus Phyllosticta ligustricola HDF-L-2 derived from the endangered conifer Pseudotsuga gaussenii

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Opportunities and Challenges for Inhibitors Targeting Citrate Transport and Metabolism in Drug Discovery

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Beshanzoides A–D, unprecedented cycloheptanone-containing polyketides from Penicillium commune P-4-1, an endophytic fungus of the endangered conifer Abies beshanzuensis

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Ácido bempedoico. Mecanismo de acción y propiedades farmacocinéticas y farmacodinámicas

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Bempedoic Acid in the Treatment of Patients with Dyslipidemias and Statin Intolerance

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Acetyl-CoA Regulation, OXPHOS Integrity and Leptin Levels Are Different in Females With Childhood vs Adulthood Onset of Obesity

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Dietary intake of bioactive ingredients impacts liver and adipose tissue transcriptomes in a porcine model of prepubertal early obesity

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Diretriz Brasileira de Dislipidemias e Prevenção da Aterosclerose – 2025

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Allosteric role of the citrate synthase homology domain of ATP citrate lyase

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Discovery of Allosteric Inhibition of Human ATP-Citrate Lyase

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ATP Citrate Lyase: A New Player Linking Skeletal Muscle Metabolism and Epigenetics

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Co-morbid intersections of cancer and cardiovascular disease and targets for natural drug action: Reprogramming of lipid metabolism

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Design, synthesis, and Biological evaluation of novel macrocyclic derivatives as potent ATP-citrate lyase inhibitors

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Recent Advances in the Genetics of Atherothrombotic Disease and Its Determinants

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Research progress and therapeutic strategies in hepatocellular carcinoma metabolic reprogramming

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Use of bempedoic acid for LDL cholesterol lowering and cardiovascular risk reduction: a consensus document from the Italian study group on atherosclerosis, thrombosis and vascular biology

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Formyl phloroglucinol meroterpenoids from the leaves of Eucalyptus globulus subsp. maidenii and their ATP-citrate lyase inhibitory activities

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ATP-CITRATE LYASEB1 supplies materials for sporopollenin biosynthesis and microspore development in Arabidopsis

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PF-05231023 reduces lipid deposition in apolipoprotein E-deficient mice by inhibiting the expression of lipid synthesis genes

Juan, Z., Liu, X., Yue, J., Zhang, S., Li, L., & Wei, H. (2024) · Frontiers in Veterinary Science · doi:10.3389/fvets.2024.1429639 · Cited by 5 · see citing works

Recent Highlights of ATVB

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Radiogenomic landscape: Assessment of specific phagocytosis regulators in lower-grade gliomas

Maimaiti, A., Abulaiti, A., Tang, B., Dilixiati, Y., Li, X., Yakufu, S., Wang, Y., Jiang, L., & Shao, H. (2023) · Experimental Biology and Medicine · doi:10.1177/15353702231211939 · Cited by 3 · see citing works

Bempedoic acid as adjunct for traditional lipid-lowering therapy in patients with hyperlipidaemia

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Metabolic profiling of bioactive components from Schizophyllum commune Fries in hypercholesterolemic Wistar-Kyoto rats using LC-QTOF-MS analysis

Sadasevevam, R., Aminudin, N., & Abdullah, N. (2025) · Prostaglandins & Other Lipid Mediators · doi:10.1016/j.prostaglandins.2025.107011 · Cited by 2 · see citing works

Role of metabolic reprogramming in colorectal cancer and pharmacologic intervention

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Comparative transcriptome and methylome of polar bears, giant and red pandas reveal diet‐driven adaptive evolution

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The use of transcriptomics to explore the mechanism of silver nanoparticle in inducing the dysregulation of cholesterol metabolism in human neural progenitor cells

Lü, Y., Wang, Y., Bao, X., Lv, X., & Huang, Y. (2025) · Ecotoxicology and Environmental Safety · doi:10.1016/j.ecoenv.2025.118152 · Cited by 2 · see citing works

The Pathogenetic Basis of the Action of Bempedoic Acid

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From common to rare: repurposing of bempedoic acid for the treatment of glycogen storage disease type 1

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Efficacy and Safety of Bempedoic Acid in Lipid Disorder Therapy: A Review of Clinical Trials

Dąbrowska, P., Żuber, M., & Dacka, M. (2024) · Prospects in Pharmaceutical Sciences · doi:10.56782/pps.208 · Cited by 1 · see citing works

ATP Citrate Lyase ClACLB-1 Facilitates Citrate Cleavage in Lemon

Lu, C., Yang, W., Zhang, H., Wu, Y., Meng, H., Lv, L., Lu, W., Zhao, D., & Huang, G. (2024) · Plants · doi:10.3390/plants14010053 · Cited by 1 · see citing works

Defining the role of bempedoic acid in lowering low-density lipoprotein cholesterol

Korzh, O. (2020) · Journal of Applied Pharmaceutical Science · doi:10.7324/japs.2020.101217 · Cited by 1 · see citing works

Atherosclerosis: Cholesterol Management

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General Perspectives for the Treatment of Atherosclerosis

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Efficacy and Safety of Bempedoic Acid in Patients with High Cardiovascular Risk: An Update

Çaklılı, Ö. T., Rizzo, M., & Cesur, M. (2024) · Current Vascular Pharmacology · doi:10.2174/0115701611290763240126045433

E2F1-driven cholesterol synthesis via the SND1/ACLY axis potentiates malignant progression in prostate cancer

Zheng, X., Yang, C., Bian, D., Shi, G., Wang, L., Li, X., Chen, Y., Xin, H., & Wang, L. (2026) · Epigenomics · doi:10.1080/17501911.2026.2617186

The ATP-Citrate Lyase Subunit ACLA, Coordinates Rice Pollen Development by Coupling Transcriptional Regulation with Metabolic Homeostasis

Li, S., Wang, H., Ye, Q., Wu, Z., Zhang, Z., Wang, X., Hu, X., Chen, J., Liu, J., Guo, D., et al. (2026) · Rice · doi:10.1186/s12284-026-00914-8

Dysregulated lipid metabolism in hepatocellular carcinoma: a review of molecular networks and therapeutic opportunities

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Aging and Cardiovascular Health: CVIA State-of-the-Art Review

Liu, N., Wang, W., Miao, R., Zhao, J., Yu, C., Hong, W., Zhao, M., Wan, Z., Peng, J., Zhang, L., et al. (2026) · Cardiovascular Innovations and Applications · doi:10.15212/cvia.2026.0009

ATP Citrate Lyase in Metabolic Disease: Mechanistic Insights and Clinical Potential

Wang, W., Li, X., Shi, H., Song, G., Xie, Z., & Li, J. (2026) · iNew Medicine · doi:10.1002/inm3.70077

Research progress on ATP-citrate lyase and its inhibitors: a metabolic-epigenetic perspective

Liu, Q., Sun, H., & Dai, L. (2026) · Journal of Enzyme Inhibition and Medicinal Chemistry · doi:10.1080/14756366.2026.2744392

BindingDB Entry 50019879: Opportunities and Challenges for Inhibitors Targeting Citrate Transport and Metabolism in Drug Discovery.

BindingDB (2024) · UC San Diego · doi:10.7270/q2k36023

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

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Targeting ATP-citrate lyase across cardiometabolic and oncologic disease

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ATP Citrate Lyase Inhibitors: A Novel Target for Treatment of Dyslipidemia

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Bempedoic acid: effects on lipoprotein metabolism and atherosclerosis

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GENETIC TARGET VALIDATION FOR ATP-CITRATE LYASE INHIBITION

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