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Jingzhaotoxin-XII, a gating modifier specific for Kv4.1 channels

机译:jin光照toxin-X II, 啊噶廷modifier specific fork V4.1 channels

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摘要

Jingzhaotoxin-XII (JZTX-XII), a 29-residue polypeptide, was purified from the venom of the Chinese tarantula Chilobrachys jingzhao. Electrophysiological recordings carried out in Xenopus laevis oocytes showed that JZTX-XII is specific for Kv4.1 channels, with the IC50 value of 0.363 mu M. It interacts with the channels by modifying the gating behavior. JZTX-XII shares 80% sequence identity with phrixotoxinl, a potent inhibitor for Kv4.2 and Kv4.3 channels. Structure analysis indicates that the difference of the charge distribution in the interactive surface perhaps influences the specific pharmacology of the toxins. JZTX-XII should be a valuable tool for the investigation of the Kv4.1 channels. (c) 2007 Published by Elsevier Ltd.
机译:景天毒素XII(JZTX-XII)是一种29个残基的多肽,是从中国捕鸟蛛Chilobrachys jingzhao的毒液中纯化得到的。在非洲爪蟾卵母细胞中进行的电生理记录表明,JZTX-XII特异于Kv4.1通道,IC50值为0.363μM。它通过修饰门控行为与通道相互作用。 JZTX-XII与phroxotoxinl共享80%的序列同一性,phrixotoxinl是Kv4.2和Kv4.3通道的有效抑制剂。结构分析表明,相互作用表面中电荷分布的差异可能会影响毒素的特定药理作用。 JZTX-XII应该是调查Kv4.1频道的有价值的工具。 (c)2007年由Elsevier Ltd.发布。

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