...
首页> 外文期刊>Proceedings of the National Academy of Sciences of the United States of America >Molecular mechanism of use-dependent calcium channel block by phenylalkylamines: Role of inactivation
【24h】

Molecular mechanism of use-dependent calcium channel block by phenylalkylamines: Role of inactivation

机译:苯烷基胺引起的依赖使用的钙通道阻滞的分子机制:失活的作用

获取原文
获取原文并翻译 | 示例
           

摘要

The role of channel inactivation in the mo- lecular mechanism of calcium (Ca~2+) channel block by phe- nylalkylamines (PAA) was analyzed by designing mutant Ca~2+ channels that carry the high affinity determinants of the PAA receptor site [Hockerman, G. H., Johnson, B. D., Scheuer, T., and Catterall, W. A. (1995) J. Biol. Chem. 270, 22119-22122] but inactivate at different rates. Use-dependent block by PAAs was studied after expressing the mutant Ca~2+ channels in Xenopus oocytes. Substitution of single putative pore- orientated amino acids in segment IIIS6 by alanine (F-1499-A, F-1500-A, F-1510-A, I-1514-A, and F-1515-A) gradually slowed channel inactivation and simultaneously reduced inhibition of barium currents (I_Ba) by (-)D600 upon depolarization by 100 ms steps at 0.1 Hz.
机译:通过设计携带PAA受体位点的高亲和力决定子的突变Ca〜2 +通道,分析了通道失活在苯基(PAA)阻断钙(Ca〜2 +)通道分子机制中的作用。 Hockerman,GH,Johnson,BD,Scheuer,T。,和Catterall,WA(1995)J.Biol.Chem。,1987。化学270,22119-22122],但以不同的速度失活。在非洲爪蟾卵母细胞中表达突变的Ca〜2 +通道后,研究了PAA的使用依赖性阻断。丙氨酸(F-1499-A,F-1500-A,F-1510-A,I-1514-A和F-1515-A)取代了IIIS6节中单个推定的孔定向氨基酸,从而逐渐减缓了通道失活并且在0.1 Hz时以100 ms的步长去极化时同时降低了(-)D600对钡电流(I_Ba)的抑制。

著录项

相似文献

  • 外文文献
  • 中文文献
  • 专利
获取原文

客服邮箱:kefu@zhangqiaokeyan.com

京公网安备:11010802029741号 ICP备案号:京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有
  • 客服微信

  • 服务号