Abstract
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. ACL is aberrantly expressed in many immortalized cells and tumors, such as breast, liver, colon, lung and prostate cancers, and is correlated reversely with tumor stage and differentiation, serving as a negative prognostic marker. ACL is an upstream enzyme of the long chain fatty acid synthesis, providing acetyl-CoA as an essential component of the fatty acid synthesis. Therefore, ACL is a key enzyme of cellular lipogenesis and potent target for cancer therapy. As a hypolipidemic strategy of metabolic syndrome and cancer treatment, many small chemicals targeting ACL have been designed and developed. This review article provides an update for the research and development of ACL inhibitors with a focus on their patent status, offering a new insight into their potential application.
Keywords: ACL inhibitors, ATP citrate lyase, cancer therapy, citrate, lipogenesis, small chemicals
Recent Patents on Anti-Cancer Drug Discovery
Title:ATP Citrate Lyase Inhibitors as Novel Cancer Therapeutic Agents
Volume: 7 Issue: 2
Author(s): Xu-Yu Zu, Qing-Hai Zhang, Jiang-Hua Liu, Ren-Xian Cao, Jing Zhong, Guang-Hui Yi, Zhi-Hua Quan and Giuseppe Pizzorno
Affiliation:
Keywords: ACL inhibitors, ATP citrate lyase, cancer therapy, citrate, lipogenesis, small chemicals
Abstract: 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. ACL is aberrantly expressed in many immortalized cells and tumors, such as breast, liver, colon, lung and prostate cancers, and is correlated reversely with tumor stage and differentiation, serving as a negative prognostic marker. ACL is an upstream enzyme of the long chain fatty acid synthesis, providing acetyl-CoA as an essential component of the fatty acid synthesis. Therefore, ACL is a key enzyme of cellular lipogenesis and potent target for cancer therapy. As a hypolipidemic strategy of metabolic syndrome and cancer treatment, many small chemicals targeting ACL have been designed and developed. This review article provides an update for the research and development of ACL inhibitors with a focus on their patent status, offering a new insight into their potential application.
Export Options
About this article
Cite this article as:
Zu Xu-Yu, Zhang Qing-Hai, Liu Jiang-Hua, Cao Ren-Xian, Zhong Jing, Yi Guang-Hui, Quan Zhi-Hua and Pizzorno Giuseppe, ATP Citrate Lyase Inhibitors as Novel Cancer Therapeutic Agents, Recent Patents on Anti-Cancer Drug Discovery 2012; 7 (2) . https://dx.doi.org/10.2174/157489212799972954
DOI https://dx.doi.org/10.2174/157489212799972954 |
Print ISSN 1574-8928 |
Publisher Name Bentham Science Publisher |
Online ISSN 2212-3970 |
Call for Papers in Thematic Issues
Novel anti-cancer drugs in photoimmunotherapy management: from bench to translational research
In recent years, traditional cancer treatments, such as surgery, chemotherapy, and radiation treatment, etc., may damage the pathological tissue and normal cells. The ideal tumor treatment should be noninvasive, eliminating the primary tumor, making the body produce systemic tumor-specific immunity, eliminating metastases, and having less /no side effects. Recent Patents ...read more
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
Noscapine and its Analogs as Chemotherapeutic Agent: Current updates
Current Topics in Medicinal Chemistry Melatonin Leads to Axonal Regeneration, Reduction in Oxidative Stress, and Improved Functional Recovery Following Sciatic Nerve Injury
Current Neurovascular Research Drug Resistance of Enzalutamide in CRPC
Current Drug Targets Medicinal Research Progress of Natural Coumarin and its Derivatives
The Natural Products Journal Effects of Liver Diseases on Drug-metabolizing Enzymes: Implications for Drug Fate Alterations and Nano-therapeutic Openings
Current Medicinal Chemistry Vitamin D - Pivotal Nutraceutical in the Regulation of Cancer Metastasis and Angiogenesis
Current Medicinal Chemistry Immunotoxicity and Immunogenicity of Biopharmaceuticals: Design Concepts and Safety Assessment
Current Drug Safety Extracts of <i>Anogeissus leiocarpus and Dillenia indica</i> Inhibit the Growth of MCF-7 Breast Cancer and COV434 Granulosa Tumor Cells by Inducing Apoptosis and Autophagy
Current Bioactive Compounds New Benzimidazole-Derived Isothioureas as Potential Antileukemic Agents - Studies <i>In Vitro</i>
Medicinal Chemistry Inhibition of TGF-β Signaling in Tumor Cells by Small Molecule Src Family Kinase Inhibitors
Anti-Cancer Agents in Medicinal Chemistry Cancer Stem Cells – Are Surface Markers Alone Sufficient?
Current Stem Cell Research & Therapy Nitric Oxide and Dietary Factors: Part III Minerals, Vitamins and Other Dietary and Lifestyle Factors
Vascular Disease Prevention (Discontinued) Pharmacokinetics of Biotech Drugs: Peptides, Proteins and Monoclonal Antibodies
Current Drug Metabolism Personalized & Precision Medicine in Cancer: A Theranostic Approach
Current Radiopharmaceuticals A Review of Ensemble Methods in Bioinformatics
Current Bioinformatics PET Imaging of Beta-Adrenoceptors in Human Brain: A Realistic Goal or a Mirage?
Current Pharmaceutical Design Brain Tumor Causes, Symptoms, Diagnosis and Radiotherapy Treatment
Current Medical Imaging Recent Advances in the Design and Development of Anticancer Molecules based on PROTAC Technology
Current Medicinal Chemistry Propargyl 4-[18F]fluorobenzoate: A Putatively More Stable Prosthetic Group for the Fluorine-18 Labeling of Biomolecules via Click Chemistry
Current Radiopharmaceuticals Fibroblast Growth Factors/Fibroblast Growth Factor Receptors as Targets for the Development of Anti-Angiogenesis Strategies
Current Pharmaceutical Design