کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10770799 | 1050835 | 2005 | 9 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Block of inactivation-deficient cardiac Na+ channels by acetyl-KIFMK-amide
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کلمات کلیدی
موضوعات مرتبط
علوم زیستی و بیوفناوری
بیوشیمی، ژنتیک و زیست شناسی مولکولی
زیست شیمی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Block of inactivation-deficient cardiac Na+ channels by acetyl-KIFMK-amide Block of inactivation-deficient cardiac Na+ channels by acetyl-KIFMK-amide](/preview/png/10770799.png)
چکیده انگلیسی
The Na+ channel α-subunit contains an IFM motif that is critical for the fast inactivation process. In this study, we sought to determine whether an IFM-containing peptide, acetyl-KIFMK-amide, blocks open cardiac Na+ channels via the inner cavity. Intracellular acetyl-KIFMK-amide at 2 mM elicited a rapid time-dependent block (Ï = 0.24 ms) of inactivation-deficient human heart Na+ channels (hNav1.5-L409C/A410W) at +50 mV. In addition, a peptide-induced tail current appeared conspicuously upon repolarization, suggesting that the activation gate cannot close until acetyl-KIFMK-amide is cleared from the open pore. Repetitive pulses (+50 mV for 20 ms at 1 Hz) produced a substantial use-dependent block of both peak and tail currents by â¼65%. A F1760K mutation (hNav1.5-L409C/A410W/F1760K) abolished the use-dependent block by acetyl-KIFMK-amide and hindered the time-dependent block. Competition experiments showed that acetyl-KIFMK-amide antagonized bupivacaine binding. These results are consistent with a model that two acetyl-KIFMK-amide receptors exist in proximity within the Na+ channel inner cavity.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Biochemical and Biophysical Research Communications - Volume 329, Issue 2, 8 April 2005, Pages 780-788
Journal: Biochemical and Biophysical Research Communications - Volume 329, Issue 2, 8 April 2005, Pages 780-788
نویسندگان
Sho-Ya Wang, Ging Kuo Wang,