The three-dimensional structure of the analgesic α-conotoxin, RgIA
The three-dimensional structure of the analgesic α-conotoxin, RgIA
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DOI：
10.1016/j.febslet.2008.01.027
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发表时间：
2008-03-05
期刊：
影响因子：
3.5
通讯作者：
Craik, David J.
中科院分区：
文献类型：
--
作者：
Clark, Richard J.;Daly, Norelle L.;Craik, David J.
α-芋螺毒素 RgIA 是 α 9 α 10 烟碱乙酰胆碱受体的选择性拮抗剂，已被证明是一种有效的镇痛剂，可减少与炎症相关的神经损伤。 RgIA 是化学合成的，发现可折叠成两种二硫键异构体：球状和带状。天然球状异构体可逆地抑制表达大鼠 α 9 α 10 nAChR 的卵母细胞中的 ACh 诱发电流，但带状异构体无活性。我们利用NMR方法测定了RgIA的三维结构，以协助阐明RgIA在镇痛和炎症中的分子作用。 (C) 2008 年欧洲生化学会联合会。由 Elsevier B.V. 出版。保留所有权利。
The alpha-conotoxin RgIA is a selective antagonist of the alpha 9 alpha 10 nicotinic acetylcholine receptor and has been shown to be a potent analgesic and reduces nerve injury associated inflammation. RgIA was chemically synthesized and found to fold into two disulfide isomers, globular and ribbon. The native globular isomer inhibited ACh-evoked currents reversibly in oocytes expressing rat alpha 9 alpha 10 nAChRs but the ribbon isomer was inactive. We determined the three-dimensional structure of RgIA using NMR methods to assist in elucidating the molecular role of RgIA in analgesia and inflammation. (C) 2008 Federation of European Biochemical Societies. Published by Elsevier B.V. All rights reserved.