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 |
- 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
-
Evaluation of a New <sup>99m</sup>Tc-labeled GnRH Analogue as a Possible Imaging Agent for Prostate Cancer Detection
Anti-Cancer Agents in Medicinal Chemistry Regulation of Angiotensin II Receptor Expression
Current Pharmaceutical Design Restoring p53 Function in Cancer: Novel Therapeutic Approaches for Applying the Brakes to Tumorigenesis
Recent Patents on Anti-Cancer Drug Discovery Multiple Functions of Mammalian Germinal Center Kinases
Current Chemical Biology Inhibition of Aurora A Kinase by Alisertib Induces Autophagy and Cell Cycle Arrest and Increases Chemosensitivity in Human Hepatocellular Carcinoma HepG2 Cells
Current Cancer Drug Targets Use of Analogs of Peptide Hormones Conjugated to Cytotoxic Radicals for Chemotherapy Targeted to Receptors on Tumors
Current Drug Delivery Personalized Peptide Vaccine for Treatment of Advanced Cancer
Current Medicinal Chemistry Dysregulation of SIRT-1 Signaling in Multiple Sclerosis and Neuroimmune Disorders: A Systematic Review of SIRTUIN Activators as Potential Immunomodulators and their Influences on other Dysfunctions
Endocrine, Metabolic & Immune Disorders - Drug Targets Emerging Concepts in the Analysis of Mitochondrial Genome Instability
Current Genomics Somatic Mutation Analyses in Studies of the Clonal Evolution and Diagnostic Targets of Prostate Cancer
Current Genomics Cellular Senescence as a Target in Cancer Control
Current Cancer Therapy Reviews Possible Predictive Value of Maspin Expression in Colorectal Cancer
Recent Patents on Anti-Cancer Drug Discovery Rational Targeting of Peroxisome Proliferating Activated Receptor Subtypes
Current Medicinal Chemistry Biology of PPARγ in Cancer: A Critical Review on Existing Lacunae
Current Molecular Medicine Antigonadotropins: A Novel Strategy to Halt Alzheimers Disease Progression
Current Pharmaceutical Design Molecular Imaging Aided Improvement in Drug Discovery and Development
Current Biotechnology CRIM1, the Antagonist of BMPs, is a Potential Risk Factor of Cancer
Current Cancer Drug Targets Fluorescent Substrates Useful as High Throughput Screening Tools for ADAM9
Combinatorial Chemistry & High Throughput Screening Recent Advances in Computer-Assisted Structure-Based Identification and Design of Histone Deacetylases Inhibitors
Current Topics in Medicinal Chemistry BUB1B Promotes Proliferation of Prostate Cancer via Transcriptional Regulation of MELK
Anti-Cancer Agents in Medicinal Chemistry