| 胰高血糖素样肽-1类似物的合成及其生物学活性研究 |
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| 引用本文： | 迟玉石,黄文龙,张惠斌,周金培,周映红,倪帅健,钱海.胰高血糖素样肽-1类似物的合成及其生物学活性研究[J].有机化学,2008,28(11):1932-1936. |
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| 作者姓名： | 迟玉石 黄文龙 张惠斌 周金培 周映红 倪帅健 钱海 |
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| 作者单位： | 中国药科大学新药研究中心,南京,210009 |
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| 摘 要： | 通过改变胰高血糖素样肽-1 (GLP-1)易被酶水解部位, 采用Fmoc/t-Bu正交保护固相合成策略, 并运用微波照射促进高效快速地合成了抗二肽基肽酶IV (DPP IV)的GLP-1类似物, 最后经过反相制备高效液相系统纯化得到目标多肽纯品. 生物学活性研究结果显示, 改造后的GLP-1类似物能有效抵抗DPP IV的水解, 并且有很好的降血糖活性. 所合成的GLP-1及其类似物的分子量和纯度均经过电喷雾质谱和高效液相确证.
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| 关 键 词： | 胰高血糖素样肽-1 二肽基肽酶IV 固相合成 微波 |
| 收稿时间： | 2008-3-12 |
| 修稿时间： | 2008-4-15 |
Synthesis and Biological Activity Studies of Glucagon-Like Peptide-1 Analogues |
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| CHI,Yu-Shi,HUANG,Wen-Long,ZHANG,Hui-Bin,ZHOU,Jin-Pei,ZHOU,Ying-Hong,NI,Shuai-Jian,QIAN,Hai.Synthesis and Biological Activity Studies of Glucagon-Like Peptide-1 Analogues[J].Chinese Journal of Organic Chemistry,2008,28(11):1932-1936. |
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| Authors: | CHI Yu-Shi HUANG Wen-Long ZHANG Hui-Bin ZHOU Jin-Pei ZHOU Ying-Hong NI Shuai-Jian QIAN Hai |
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| Institution: | (Center of Drug Research, China Pharmaceutical University, Nanjing 210009) |
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| Abstract: | Glucagon-like peptide-1 (GLP-1) analogues were designed through the modification of the en- zymatic hydrolyzation position. The synthesis of GLP-1 analogues was implemented rapidly and efficiently under microwave irradiation, using Fmoc/t-Bu orthogonal protection solid phase strategy. The crude peptides were purified by preparative RP-HPLC. The results of biological activity research showed that the GLP-1 analogues had great resistance to the degradation by dipeptidyl peptidase (DPP IV) and decreased the blood glucose prominently. The molecular weight and purity of the GLP-1 analogues have been confirmed through the electrospray mass spectrometry analysis and the HPLC analysis. |
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| Keywords: | GLP-1 DPP IV solid phase synthesis microwave |
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