Chemical synthesis and characterization of two alpha 4/7-conotoxins
文献类型：期刊论文
| 作者 | Peng, C; Chen, WH; Sanders, T; Chew, G; Liu, J; Hawrot, E; Chi, CW |
| 刊名 | ACTA BIOCHIMICA ET BIOPHYSICA SINICA
 |
| 出版日期 | 2010 |
| 卷号 | 42期号:10页码:745-753 |
| 关键词 | Conus alpha 4 7-conotoxin nicotinic acetylcholine receptor analgesic |
| 通讯作者 | Chi, CW (reprint author), Tongji Univ, Coll Life Sci & Technol, Inst Prot Res, Shanghai 200092, Peoples R China.,zwqi@sibs.ac.cn |
| 英文摘要 | alpha-Conotoxins are small disulfide-constrained peptides that act as potent and selective antagonists on specific subtypes of nicotinic acetylcholine receptors (nAChRs). We previously cloned two alpha-conotoxins, Mr1.1 from the molluscivorous Conus marmoreus and Lp1.4 from the vermivorous Conus leopardus. Both of them have the typical 4/7-type framework of the subfamily of alpha-conotoxins that act on neuronal nAChRs. In this work, we chemically synthesized these two toxins and characterized their functional properties. The synthetic Mr1.1 could primarily inhibit acetylcholine (ACh)-evoked currents reversibly in the oocyte-expressed rat alpha 7 nAChR, whereas Lp1.4 was an unexpected specific blocker of the mouse fetal muscle alpha 1 beta 1 gamma delta receptor. Although their inhibition affinities were relatively low, their unique receptor recognition profiles make them valuable tools for toxin-receptor interaction studies. Mr1.1 could also suppress the inflammatory response to pain in vivo, suggesting that it should be further investigated with respect to its molecular role in analgesia and its mechanism or therapeutic target for the treatment of pain. |
| 学科主题 | Biochemistry & Molecular Biology; Biophysics |
| 类目[WOS] | Biochemistry & Molecular Biology ; Biophysics |
| 关键词[WOS] | NICOTINIC ACETYLCHOLINE-RECEPTORS ; 1.1 ANGSTROM RESOLUTION ; ALPHA-CONOTOXINS IMI ; CALCIUM-CHANNELS ; SUBTYPE SELECTIVITY ; CONUS-EPISCOPATUS ; CRYSTAL-STRUCTURE ; CHROMAFFIN CELLS ; IN-VITRO ; N-TYPE |
| 收录类别 | SCI |
| 语种 | 英语 |
| WOS记录号 | WOS:000282166500009 |
| 版本 | 出版稿 |
| 源URL | [http://202.127.25.143/handle/331003/1056]  |
| 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 | Peng, C,Chen, WH,Sanders, T,et al. Chemical synthesis and characterization of two alpha 4/7-conotoxins[J]. ACTA BIOCHIMICA ET BIOPHYSICA SINICA,2010,42(10):745-753. |
| APA | Peng, C.,Chen, WH.,Sanders, T.,Chew, G.,Liu, J.,...&Chi, CW.(2010).Chemical synthesis and characterization of two alpha 4/7-conotoxins.ACTA BIOCHIMICA ET BIOPHYSICA SINICA,42(10),745-753. |
| MLA | Peng, C,et al."Chemical synthesis and characterization of two alpha 4/7-conotoxins".ACTA BIOCHIMICA ET BIOPHYSICA SINICA 42.10(2010):745-753. |
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