A NEW FAMILY OF CONUS PEPTIDES TARGETED TO THE NICOTINIC ACETYLCHOLINE-RECEPTOR
A NEW FAMILY OF CONUS PEPTIDES TARGETED TO THE NICOTINIC ACETYLCHOLINE-RECEPTOR
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DOI：
10.1074/jbc.270.38.22361
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发表时间：
1995-09-22
影响因子：
4.8
通讯作者：
OLIVERA, BM
中科院分区：
文献类型：
--
作者：
HOPKINS, C;GRILLEY, M;OLIVERA, BM
本工作定义了一个新的芋螺肽家族--α-A-芋螺毒素，它靶向烟碱乙酰胆碱受体，该家族的第一个成员已从东太平洋物种--紫芋螺（Conus purpurascens）中鉴定出来（紫色圆锥体）;从牛奶毒液中纯化并表征了三种引起鱼麻痹的肽，其中之一，α A-芋螺毒素PIVA，式中O表示反式4-羟基脯氨酸。另外两种从C. Purpurascens蛇毒中的α-A-芋螺毒素（[Pro（13）]alpha A-conotoxin PIVA）和α-A-芋螺毒素（[Pro（7，13）]alpha A-conotoxin PNA）是两种具有生物活性的多肽，电生理实验和与α-银环蛇毒素的竞争结合实验均表明，α-A-PIVA是突触后膜烟碱型乙酰胆碱受体的拮抗剂。
In this work, a new family of Conus peptides, the alpha A-conotoxins, which target the nicotinic acetylcholine receptor, is defined, The first members of this family have been characterized from the eastern Pacific species, Conus purpurascens (the purple cone); three peptides that cause paralysis in fish were purified and characterized from milked venom, The sequence and disulfide bonding pattern of one of these, alpha A-conotoxin PIVA, is as follows:[GRAPHICS]where O represents trans 4-hydroxyproline. The two other peptides purified from C. purpurascens venom are the under-hydroxylated derivatives, [Pro(13)]alpha A-conotoxin PIVA and [Pro(7,13)]alpha A-conotoxin PNA.The peptides have been chemically synthesized in a biologically active form, Both electrophysiological experiments and competition binding with alpha-bungarotoxin demonstrate that alpha A-PIVA acts as an antagonist of the nicotinic acetylcholine receptor at the postsynaptic membrane.