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

Luo, D. X., Tong, D. J., Rajput, S., Wang, C., Liao, D. F., Cao, D. L. and Maser, Edmund (2012) Targeting Acetyl-CoA Carboxylases: Small Molecular Inhibitors and their Therapeutic Potential Recent Patents on Anti-Cancer Drug Discovery, 7 (2). pp. 168-184.

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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.

Document Type: Article
Additional Information: Univ Med Sch Schleswig Holstein, Inst Toxicol & Pharmacol Nat Scientists, D-24105 Kiel, Germany. First Peoples Hosp Chenzhou, Inst Translat Med, Chenzhou 423000, Hunan, Peoples R China. First Peoples Hosp Chenzhou, Dept Lab Med, Chenzhou 423000, Hunan, Peoples R China. So Illinois Univ, Sch Med, Simmons Canc Inst, Dept Microbiol Immunol & Cell Biol, Springfield, IL 62794 USA. Cent Hosp Yiyang, Dept Cardiovasc Med, Yiyang 41300, Peoples R China. Univ S China, Coll Pharmaceut & Life Sci, Inst Pharm & Pharmacol, Hengyang 421001, Peoples R China. Hunan Univ Chinese Med, Sch Pharm, Dept Tradit Chinese Diagnot, Changsha 420108, Hunan, Peoples R China. Maser, E (reprint author), Univ Med Sch Schleswig Holstein, Inst Toxicol & Pharmacol Nat Scientists, Campus Kiel,Brunswiker Str 10, D-24105 Kiel, Germany. maser@toxi.uni-kiel.de
Keywords: Acetyl-CoA carboxylases cancer fatty acid synthesis inhibitors metabolic syndromes obesity fatty-acid synthase coenzyme-a carboxylase activated protein-kinase streptomyces-coelicolor a3(2) breast-cancer cells biosynthetic gene-cluster hypothalamic malonyl-coa parental species cloning affects lipid-synthesis coronary-heart-disease
Research affiliation: OceanRep > The Future Ocean - Cluster of Excellence
Kiel University
ISSN: 1574-8928
Projects: Future Ocean
Date Deposited: 14 May 2014 09:49
Last Modified: 14 May 2014 09:49
URI: http://eprints.uni-kiel.de/id/eprint/24105

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