Model studies of the function of blockers on the small conductance potassium ion channel.
A correlation between KI (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.
Ciechanowicz-Rutkowska
M
M
Regional Laboratory for Physicochemical Research and Structural Analysis, Ingardena 3, 30-060 Krakow, Poland.
Lewinski
K
K
Oleksyn
B
B
Stec
B
B
D001030:Apamin / Q000737:chemistry* / Q000494:pharmacology*; D002118:Calcium / Q000378:metabolism; D008958:Models, Molecular; D008968:Molecular Conformation; D026902:Potassium Channel Blockers / Q000737:chemistry / Q000494:pharmacology*; D015221:Potassium Channels / Q000187:drug effects*; D013223:Statistics as Topic
D026902:Potassium Channel Blockers; D015221:Potassium Channels; D001030:Apamin; D002118:Calcium