| 用于治疗肥胖和糖尿病的二酰甘油酰基转移酶抑制剂研究进展 |
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| 引用本文： | 王吉超,孙宏斌. 用于治疗肥胖和糖尿病的二酰甘油酰基转移酶抑制剂研究进展[J]. 药学进展, 2012, 36(2): 57-64 |
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| 作者姓名： | 王吉超 孙宏斌 |
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| 作者单位： | 中国药科大学新药研究中心,江苏南京,210009 |
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| 摘 要： | 人体内的二酰甘油酰基转移酶是催化三酰甘油最终合成的关键酶，其基因缺失或酶活受抑时，机体不会因高脂饮食而发生肥胖，且对胰岛素的敏感性增强，因此该酶可作为肥胖和糖尿病治疗药物的靶点。综述二酰甘油酰基转移酶的功能研究以及天然来源和合成的二酰甘油酰基转移酶抑制剂的药理活性和构效关系。
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| 关 键 词： | 二酰甘油酰基转移酶抑制剂 三酰甘油 2型糖尿病 肥胖 |
Advances in Research on Diacylglycerol Acyltransferase Inhibitors in the Treatment of Obesity and Diabetes Mellitus |
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| WANG Ji-chao , SUN Hong-bin. Advances in Research on Diacylglycerol Acyltransferase Inhibitors in the Treatment of Obesity and Diabetes Mellitus[J]. Progress in Pharmaceutical Sciences, 2012, 36(2): 57-64 |
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| Authors: | WANG Ji-chao SUN Hong-bin |
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| Affiliation: | (Center of Drug Discovery,China Pharmaceutical University,Nanjing 210009,China) |
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| Abstract: | Diacylglycerol acyltransferases(DGATs) are the key enzymes which catalyze the final step of the triglyceride synthesis.DGAT gene defect and inhibition of DGATs can prevent obesity induced by high-fat diet and increase the sensitivity of organisms to insulin,so DGATs may be an ideal target in the treatment of obesity and type 2 diabetes mellitus.The biological functions of DGATs,as well as the pharmacological activities and structure-activity relationships(SARs) of natural and synthesized DGATs inhi-bitors were reviewed in this paper. |
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| Keywords: | diacylglycerol acyltransferase inhibitor triglyceride type 2 diabetes mellitus obesity |
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