Inhibition of martentoxin on neuronal BK channel subtype (alpha+beta4): implications for a novel interaction model

Biophysical Journal
Jian ShiYong Hua Ji

Abstract

Martentoxin as a 37-residue peptide was capable of blocking large-conductance Ca(2+)-activated K(+) (BK) channels in adrenal medulla chromaffin cells. This study investigated the pharmacological discrimination of martentoxin on BK channel subtypes. The results showed that the iberiotoxin-insensitive neuronal BK channels (alpha+beta4) could be potently blocked by martentoxin (IC(50) = approximately 80 nM). In contrast, the iberiotoxin-sensitive BK channel consisting of only alpha-subunit was less sensitive to martentoxin. Distinctively, martentoxin inhibited neuronal BK channels (alpha+beta4) with a novel interaction mode. Two possible interaction sites of neuronal BK channels (alpha+beta4) might be responsible for the binding with martentoxin: one for trapping and the other located at the pore region for blocking. In addition, the inhibition of martentoxin on neuronal BK channels (alpha+beta4) depended on cytoplasmic Ca(2+) concentration. On the other hand, in vivo experiments from EEG recordings suggested that neuronal BK channels (alpha+beta4) were the primary target of martentoxin. Therefore, this research not only sheds light on a unique ligand for neuronal BK channels (alpha+beta4), but also highlights a novel model approa...Continue Reading

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Citations

Mar 1, 2014·Toxins·Zhijian CaoWenxin Li
Jan 5, 2016·Acta Pharmacologica Sinica·Mu YuLong-hua Zhang
Oct 28, 2014·Frontiers in Physiology·Bin WangRobert Brenner
Oct 28, 2014·Frontiers in Physiology·Yolima P TorresRamón Latorre
Mar 24, 2020·Investigative Ophthalmology & Visual Science·Jacques A BertrandDarryl R Overby
Nov 4, 2016·Physiological Reviews·Ramon LatorreOsvaldo Alvarez
Jun 22, 2021·The Journal of Venomous Animals and Toxins Including Tropical Diseases·Xiaoli WangJie Tao
Dec 17, 2019·Journal of Medicinal Chemistry·Xinlian LiuChunyang Cao
Oct 30, 2016·Neuropharmacology·David M HousleyErnest A Jennings
Apr 7, 2011·Comparative Biochemistry and Physiology. Part A, Molecular & Integrative Physiology·Bin GaoShunyi Zhu

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