Structural basis of binding and inhibition of novel tarantula toxins in mammalian voltage-dependent potassium channels.

作者: Yu-Shuan Shiau , Po-Tsang Huang , Horng-Huei Liou , Yen-Chywan Liaw , Yuh-Yuan Shiau

DOI: 10.1021/TX0341097

关键词:

摘要: Voltage-dependent potassium channel Kv2.1 is widely expressed in mammalian neurons and was suggested responsible for mediating the delayed rectifier (IK) currents. Further investigation of central role this requires development specific pharmacology, instance, utilization spider venom toxins. Most these toxins belong to same structural family with a short peptide reticulated by disulfide bridges share similar mode action. Hanatoxin 1 (HaTx1) from Chilean tarantula one earliest discussed tools regarding has been intensively applied characterize blocking not through pore domain. Recently, more related novel African tarantulas such as heteroscordratoxins (HmTx) stromatoxin (ScTx1) were isolated shown act gating modifiers HaTx on channels electrophysiological recordings. However, further interaction details are unavailable due lack high-resolution structures vol...

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