Targeting Acetyl-CoA Carboxylases: Small Molecular Inhibitors and their Therapeutic Potential

Author(s): Di-Xian Luo, Di-Jun Tong, Sandeep Rajput, Chun Wang, Duan-Fang Liao, Deliang Cao, Edmund Maser.

Journal Name: Recent Patents on Anti-Cancer Drug Discovery

Volume 7 , Issue 2 , 2012

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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

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Article Details

VOLUME: 7
ISSUE: 2
Year: 2012
Page: [168 - 184]
Pages: 17
DOI: 10.2174/157489212799972918
Price: $58

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