Effect of human serum albumin on drug metabolism: Structural evidence of esterase activity of human serum albumin
文献类型：期刊论文
| 作者 | F. Yang ; C. B. Bian ; L. L. Zhu ; G. X. Zhao ; Z. X. Huang ; M. D. Huang |
| 刊名 | Journal of Structural Biology
 |
| 出版日期 | 2007-02 |
| 卷号 | 157期号:2页码:348-355 |
| 关键词 | human serum albumin drug metabolism aspirin salicylic acid esterase activity structure acetylsalicylic-acid crystal-structure ligand-binding nitrophenyl esters acetylation aspirin resolution chemistry reveals sites |
| ISSN号 | 1047-8477 |
| 中文摘要 | Human serum albumin (HSA) is the most abundant plasma protein in the human body with a plasma concentration of 0.6 mM. HSA plays an important role in drug transport and metabolism. Enzymatic activity of HSA on different substrates or drugs has been studied and documented. The structural mechanism of this activity, however, is unknown. In this study, we have determined the crystal structures of HSA-myristate in a complex of aspirin and of salicylic acid, respectively. The crystal structure of HSA myristate-aspirin illustrates that aspirin transfers acetyl group to Lys199 and is hydrolyzed into salicylic acid by HSA. The hydrolysis product, salicylic acid, remains bound to HSA at a similar location, but it shows a very different orientation when compared with the salicylic acid in the HSA-myristate-salicylic acid ternary complex. These results not only provide the structural evidence of esterase activity of HSA, and demonstrate the conformational plasticity of HSA on drug binding, but also may provide structural information for the modulation of HSA-drug interaction by computational approach based on HSA-drug structure. (c) 2006 Elsevier Inc. All rights reserved. |
| 语种 | 英语 |
| 公开日期 | 2013-04-01 |
| 源URL | [http://ir.fjirsm.ac.cn/handle/350002/6797]  |
| 专题 | 福建物质结构研究所_中科院福建物质结构研究所_期刊论文 |
| 推荐引用方式 GB/T 7714 | F. Yang,C. B. Bian,L. L. Zhu,et al. Effect of human serum albumin on drug metabolism: Structural evidence of esterase activity of human serum albumin[J]. Journal of Structural Biology,2007,157(2):348-355. |
| APA | F. Yang,C. B. Bian,L. L. Zhu,G. X. Zhao,Z. X. Huang,&M. D. Huang.(2007).Effect of human serum albumin on drug metabolism: Structural evidence of esterase activity of human serum albumin.Journal of Structural Biology,157(2),348-355. |
| MLA | F. Yang,et al."Effect of human serum albumin on drug metabolism: Structural evidence of esterase activity of human serum albumin".Journal of Structural Biology 157.2(2007):348-355. |
入库方式： OAI收割
来源：福建物质结构研究所
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