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| 脂肪酸结合蛋白4小分子抑制剂研究进展 | |
| 引用本文： | 刘璐,张鸣鸣,李英霞,孟艳秋. 脂肪酸结合蛋白4小分子抑制剂研究进展[J]. 中国药物化学杂志, 2013, 0(5): 400-405,416 |
| 作者姓名： | 刘璐 张鸣鸣 李英霞 孟艳秋 |
| 作者单位： | [1]沈阳化工大学制药与生物工程学院制药工程教研室,辽宁沈阳110142 [2]复旦大学药学院药物化学教研室,上海201203 |
| 摘 要： | 存在于脂肪细胞和巨噬细胞中的脂肪酸结合蛋白4(FABP4)能够调节炎症和新陈代谢。研究表明,脂肪酸结合蛋白与新陈代谢综合征、炎症、动脉粥样硬化等疾病的发生存在密切联系。FABP还能够提高胰岛素的敏感性,因而也是治疗2型糖尿病的潜在靶标。本文从化学结构、生物活性、选择性以及构效关系等方面对目前已报道的FABP4小分子抑制剂的研究进行综述。 |
| 关 键 词： | 脂肪酸结合蛋白4 抑制剂 小分子 选择性 2型糖尿病 |
Evolution of design and development of FABP4 inhibitors |
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| LIU Lu,ZHANG Ming-ming,LI Ying-xia,MENG Yan-qiu. Evolution of design and development of FABP4 inhibitors[J]. Chinese Journal of Medicinal Chemistry, 2013, 0(5): 400-405,416 | |
| Authors: | LIU Lu ZHANG Ming-ming LI Ying-xia MENG Yan-qiu |
| Affiliation: | 1. Department of Medicinal Chemistry, School of Chemical Engineering ,Shenyang University of Chemical Technology, Shenyang 110142, China ; 2. Department of Medicinal Chemistry, School of Pharmacy, Fudan University, Shanghai 201203, China) |
| Abstract: | Fatty acid binding protein 4 （ FABP4 ） can modulate inflammatory and metabolic response, and it is expressed in adipocytes and macrophage. The inhibitors can improve insulin sensitivity and resistance to the development of atherosclerosis, and is a potential target for the treatment of type 2 diabetes. Up to now a series of potent small molecule inhibitors of FABP4 which are potential to prevent and treat metabolic diseases such as atherosclerosis and type 2 diabetes have been identified and found. Base on the literature of the recent years, the main inhibitors were discussed emphasizing particularly on chemical structures, biological properties, selectivity and structure-activity relationships in this review. |
| Keywords: | fatty acid binding protein 4 inhibitor small molecule selectivity type 2 diabetes |
| 本文献已被 CNKI 维普 等数据库收录！ | |