Isosteric replacement of A3 Val of porcine insulin by allo-Thr
文献类型：期刊论文
| 作者 | Li, MY; Cui, DF; Zhang, YS |
| 刊名 | IUBMB LIFE
 |
| 出版日期 | 2002 |
| 卷号 | 53期号:1页码:57-60 |
| 关键词 | A3 allo-Thr insulin isosteric interaction peptide synthesis receptor binding semisynthesis |
| 通讯作者 | Zhang, YS (reprint author), Chinese Acad Sci, Shanghai Inst Biol Sci, Shanghai Inst Biochem & Cell Biol, Shanghai 200031, Peoples R China., |
| 英文摘要 | A3 Val is important for insulin activity. It is invariant in insulins from different species studied thus far. Based on the three dimensional structure of insulin, it was thought to be involved in receptor binding. Its replacement by Leu resulted in remarkable lowering of insulin activity, indicating the crucial requirement of the side chain geometry at this position. When A3 Val was replaced by Thr, which is hydrophilic but isosteric with Val, substantial insulin activity was retained. Therefore, the isosteric requirement for receptor binding at this site is more stringent than the hydrophobic requirement. Here we report the replacement of A3 Val of porcine insulin by the unnatural allo-Thr. The in vivo biological activity of A3 allo-Thr insulin is similar to that of A3 Thr insulin or native insulin, but its receptor binding activity is 7.6% instead of 50% for A3 Thr insulin, indicating that at the A3 position the hydrophilic OH group of Thr could be more tolerated in receptor binding than the OH group of allo-Thr. The retention of insulin activity by substituting A3 Val with the unnatural isosteric allo-Thr demonstrates again the importance of isosteric interaction in the binding of insulin with its receptor. |
| 学科主题 | Biochemistry & Molecular Biology; Cell Biology |
| 类目[WOS] | Biochemistry & Molecular Biology ; Cell Biology |
| 关键词[WOS] | BINDING |
| 收录类别 | SCI |
| 语种 | 英语 |
| WOS记录号 | WOS:000175201700008 |
| 版本 | 出版稿 |
| 源URL | [http://202.127.25.143/handle/331003/2429]  |
| 专题 | 上海生化细胞研究所_上海生科院生化细胞研究所 |
| 推荐引用方式 GB/T 7714 | Li, MY,Cui, DF,Zhang, YS. Isosteric replacement of A3 Val of porcine insulin by allo-Thr[J]. IUBMB LIFE,2002,53(1):57-60. |
| APA | Li, MY,Cui, DF,&Zhang, YS.(2002).Isosteric replacement of A3 Val of porcine insulin by allo-Thr.IUBMB LIFE,53(1),57-60. |
| MLA | Li, MY,et al."Isosteric replacement of A3 Val of porcine insulin by allo-Thr".IUBMB LIFE 53.1(2002):57-60. |
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