Institute of Translational Medicine & Department of Laboratory Medicine, The First People's Hospital of Chenzhou, Chenzhou, Hunan, PR China.
Recent Pat Anticancer Drug Discov. 2012 May 1;7(2):168-84. doi: 10.2174/157489212799972918.
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.
乙酰辅酶 A 羧化酶（ACCs）在植物、微生物、哺乳动物和人类的脂肪酸生物合成中起限速作用。ACCs 具有生物素羧化酶（BC）和羧基转移酶（CT）的活性，催化乙酰辅酶 A 羧化为丙二酰辅酶 A。在过去的几年中，ACCs 已被用作农业除草剂的靶点，也被用于药物发现和人类疾病的治疗，如微生物感染、糖尿病、肥胖和癌症。已经开发出大量的小分子 ACC 抑制剂，包括天然和非天然（人工）产物。这些化学物质靶向 BC 反应、CT 反应或 ACC 磷酸化。本文全面综述了 ACC 抑制剂，并重点讨论了它们在代谢综合征和恶性疾病中的治疗应用。讨论了常见 ACC 抑制剂的专利状况。
