Abstract
Acetyl-CoA carboxylases (ACCs) play a rate-limiting role in fatty acid biosynthesis in plants, microbes, mammals and humans. ACCs have the activity of both biotin carboxylase (BC) and carboxyltransferase (CT), catalyzing carboxylation of Acetyl-CoA to malonyl-CoA. In the past years, ACCs have been used as targets for herbicides in agriculture and for drug discovery and development of human diseases, such as microbial infections, diabetes, obesity and cancer. A great number of small molecule ACC inhibitors have been developed, including natural and non-natural (artificial) products. These chemicals target BC reaction, CT reaction or ACC phosphorylation. This article provides a comprehensive review and updates of ACC inhibitors, with a focus on their therapeutic application in metabolic syndromes and malignant diseases. The patent status of common ACC inhibitors is discussed.
Keywords: Acetyl-CoA carboxylases, cancer, fatty acid synthesis, inhibitors, metabolic syndromes, obesity
Recent Patents on Anti-Cancer Drug Discovery
Title:Targeting Acetyl-CoA Carboxylases: Small Molecular Inhibitors and their Therapeutic Potential
Volume: 7 Issue: 2
Author(s): Di-Xian Luo, Di-Jun Tong, Sandeep Rajput, Chun Wang, Duan-Fang Liao, Deliang Cao and Edmund Maser
Affiliation:
Keywords: Acetyl-CoA carboxylases, cancer, fatty acid synthesis, inhibitors, metabolic syndromes, obesity
Abstract: Acetyl-CoA carboxylases (ACCs) play a rate-limiting role in fatty acid biosynthesis in plants, microbes, mammals and humans. ACCs have the activity of both biotin carboxylase (BC) and carboxyltransferase (CT), catalyzing carboxylation of Acetyl-CoA to malonyl-CoA. In the past years, ACCs have been used as targets for herbicides in agriculture and for drug discovery and development of human diseases, such as microbial infections, diabetes, obesity and cancer. A great number of small molecule ACC inhibitors have been developed, including natural and non-natural (artificial) products. These chemicals target BC reaction, CT reaction or ACC phosphorylation. This article provides a comprehensive review and updates of ACC inhibitors, with a focus on their therapeutic application in metabolic syndromes and malignant diseases. The patent status of common ACC inhibitors is discussed.
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Luo Di-Xian, Tong Di-Jun, Rajput Sandeep, Wang Chun, Liao Duan-Fang, Cao Deliang and Maser Edmund, Targeting Acetyl-CoA Carboxylases: Small Molecular Inhibitors and their Therapeutic Potential, Recent Patents on Anti-Cancer Drug Discovery 2012; 7 (2) . https://dx.doi.org/10.2174/157489212799972918
DOI https://dx.doi.org/10.2174/157489212799972918 |
Print ISSN 1574-8928 |
Publisher Name Bentham Science Publisher |
Online ISSN 2212-3970 |
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