کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
5372396 | 1388877 | 2006 | 11 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Interaction of local anesthetics with a peptide encompassing the IV/S4-S5 linker of the Na+ channel
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کلمات کلیدی
LDCSDSBZCDSSNOESYTOCSYHSQCtrifluoroethanolTFEnuclear magnetic resonance - رزونانس مغناطیسی هستهایNuclear Overhauser Effect SpectroscopY - Spectroscopy اثر Overhauser هسته ایBenzocaine - بنزوکائینLocal anesthetics - بی حسکننده موضعیNMR - تشدید مغناطیسی هستهای Diffusion Ordered SpectroscopY - توزیع شده توسط SpectroscopY مرتب شده استcircular dichroism - رنگ تابی دورانیsodium dodecyl-sulfate - سدیم دودسیل سولفاتTotal correlation spectroscopy - طیف سنجی مجموع همبستگیcorrelation spectroscopy - طیف سنجی همبستگیDOSY - فایلLidocaine - لیدوکائینPeptide - پپتید voltage-gated sodium channel - کانال سدیم ولتاژCOSY - کثیفheteronuclear single quantum coherence - یکپارچگی کوانتومی تک هسته ای
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی تئوریک و عملی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Interaction of local anesthetics with a peptide encompassing the IV/S4-S5 linker of the Na+ channel Interaction of local anesthetics with a peptide encompassing the IV/S4-S5 linker of the Na+ channel](/preview/png/5372396.png)
چکیده انگلیسی
The peptide pIV/S4-S5 encompasses the cytoplasmic linker between helices S4-S5 in domain IV of the voltage-gated Na+ channel, residues 1644-1664.2 The interaction of two local anesthetics (LA), lidocaine and benzocaine, with pIV/S4-S5 has been studied by DOSY, heteronuclear NMR 1H-15N-HSQC spectroscopy and computational methods. DOSY indicates that benzocaine, a neutral ester, exhibits stronger interaction with pIV/S4-S5 than lidocaine, a charged amine-amide. Weighted average chemical shifts, Îδ(1H-15N), show that benzocaine affects residues L1653, M1655 and S1656 while lidocaine slightly perturbs residues I1646, L1649 and A1659, L1660, near the N- and C-terminus, respectively. Computational methods confirmed the stability of the benzocaine binding and the existence of two binding sites for lidocaine. Even considering that the approach of studying the peptide in the presence of a co-solvent (TFE/H2O, 30%/70% v/v) has an inherently limited implication, our data strongly support the existence of multiple LA binding sites in the IV/S4-S5 linker, as suggested in the literature. In addition, we consider that LA can bind to the S4-S5 linker with diverse binding modes and strength since this linker is part of the receptor for the “inactivation gate particle”. Conditions for devising new functional studies, aiming to better understand Na+ channel functionality as well as the various facets of LA pharmacological activity are proposed in this work.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Biophysical Chemistry - Volume 123, Issue 1, 20 August 2006, Pages 29-39
Journal: Biophysical Chemistry - Volume 123, Issue 1, 20 August 2006, Pages 29-39
نویسندگان
Leonardo F. Fraceto, Sérgio Jr., Clóvis R. Nakaie, Alberto Spisni, Eneida de Paula, Thelma A. Pertinhez,