On site of action of grayanotoxin in domain 4 segment 6 of rat skeletal muscle sodium channel
FEBS letters 465 巻 1 号
18-22 頁
2000-01-07 発行
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| ファイル情報(添付) | |
| タイトル ( eng ) |
On site of action of grayanotoxin in domain 4 segment 6 of rat skeletal muscle sodium channel
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| 作成者 |
Kimura Takahiro
Yamaoka Kaoru
Yuki Tsunetsugu
Yakehiro Masuhide
Seyama Issei
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| 収録物名 |
FEBS letters
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| 巻 | 465 |
| 号 | 1 |
| 開始ページ | 18 |
| 終了ページ | 22 |
| 抄録 |
Grayanotoxin I (GTX I) is a diterpenoid extracted from the family of Ericaceae that binds to Na+ channels and causes persistent activation. We investigated the interaction of GTX I with the amino acid residues I1575, F1579 and Y1586 in transmembrane segment D4S6 of μ1. In F1579A, GTX shifted the threshold potential about 50 mV in the hyperpolarizing direction and modified Na+ channels twice as efficiently as that in WT. In contrast, these GTX effects were eliminated completely in the I1575A mutant and were reduced substantially in mutant Y1586A. Lysine substitution for F1579 significantly reduced and for Y1586 completely eradicated the GTX-effect. Our data suggest that the GTX receptor site shares overlapping but not-identical molecular determinants with BTX in D4S6 as well as having common molecular determinants in D1S6.
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| 著者キーワード |
grayanotoxin
binding site
Na+ channel
batrachotoxin
domain 4 segment 6
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| NDC分類 |
生物科学・一般生物学 [ 460 ]
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| 言語 |
英語
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| 資源タイプ | 学術雑誌論文 |
| 出版者 |
Elsevier
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| 発行日 | 2000-01-07 |
| 権利情報 |
Copyright (c) 2000 Federation of European Biochemical Societies. Published by Elsevier Science B.V.
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| 出版タイプ | Author’s Original（十分な品質であるとして、著者から正式な査読に提出される版） |
| アクセス権 | オープンアクセス |
| 収録物識別子 |
[ISSN] 0014-5793
[DOI] 10.1016/S0014-5793(99)01715-9
[NCID] AA00642943
[PMID] 10620699
[DOI] http://dx.doi.org/10.1016/S0014-5793(99)01715-9
～の異版である
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