Model studies of the function of blockers on the small conductance potassium ion channel

被引:2
作者
Ciechanwicz-Rutkowska, C
Lewinski, K
Oleksyn, B
Stec, B
机构
[1] Univ Texas, Dept Chem, El Paso, TX 79968 USA
[2] Reg Lb Physicochem Res & Struct Anal, PL-30060 Krakow, Poland
[3] Jagiellonian Univ, Fac Chem, PL-30060 Krakow, Poland
[4] Univ Texas, Dept Chem, El Paso, TX 79968 USA
来源
JOURNAL OF PEPTIDE RESEARCH | 2003年 / 62卷 / 03期
关键词
apamin; ion channels; ion channel blockers; NEUROMUSCULAR BLOCKING-AGENT; NUCLEAR MAGNETIC-RESONANCE; CRYSTAL-STRUCTURE; MOLECULAR-STRUCTURE; 3-DIMENSIONAL STRUCTURE; PRIORI CALCULATION; METHANOL SOLVATE; K+ CHANNELS; BEE VENOM; APAMIN;
D O I
10.1034/j.1399-3011.2003.00076.x
中图分类号
Q5 [生物化学];
学科分类号
071010 ; 081704 ;
摘要
A correlation between K-1 (equilibrium dissociation constants) and IC50 (concentration at 50% inhibition) inhibitors for the family of blockers of the small conductance potassium ion channels and their intrinsic characteristics like molecular mass and volume have been investigated. Most of the blockers in the family are not selective, in contrast to apamin - an 18 amino acid bee venom toxin -that is known to-be a highly potent and selective blocker of these channels. Differences and similarities between the blockers have been analyzed, pointing toward the origin of their selectivity and relative potency. In conclusion, an ion channel blocking is a process controlled mainly by diffusion, in accordance with previous experimental results.
引用
收藏
页码:125 / 133
页数:9
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