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Inhibition of martentoxin on neuronal BK channel subtype (alpha+beta 4): Implications for a novel interaction model
Shi, Jian2; He, Hui Qiong2; Zhao, Rong2; Duan, Yan-Hong1; Chen, Jin2; Chen, Ying1; Yang, Juan1; Zhang, Jian Wei1; Shu, Xue Qin1; Zheng, Ping3; Ji, Yong Hua1
Corresponding AuthorJi, Yong Hua(yhji@staff.shu.edu.cn)
2008-05-01
Source PublicationBIOPHYSICAL JOURNAL
ISSN0006-3495
Volume94Issue:9Pages:3706-3713
AbstractMartentoxin as a 37-residue peptide was capable of blocking large-conductance Ca2+- 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+beta 4)) could be potently blocked by martentoxin (IC50=similar to 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+beta 4) with a novel interaction mode. Two possible interaction sites of neuronal BK channels ( alpha+beta 4) 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+beta 4) depended on cytoplasmic Ca2+ concentration. On the other hand, in vivo experiments from EEG recordings suggested that neuronal BK channels ( alpha+beta 4) were the primary target of martentoxin. Therefore, this research not only sheds light on a unique ligand for neuronal BK channels ( alpha+beta 4), but also highlights a novel model approach for the interaction between K 1 channels and specific-ligands.
Indexed BySCI
Language英语
WOS Research AreaBiophysics
WOS SubjectBiophysics
WOS IDWOS:000254829700031
PublisherBIOPHYSICAL SOC
Citation statistics
Cited Times:21[WOS]   [WOS Record]     [Related Records in WOS]
Document Type期刊论文
Identifierhttp://ir.imr.ac.cn/handle/321006/93369
Collection中国科学院金属研究所
Corresponding AuthorJi, Yong Hua
Affiliation1.Shanghai Univ, Sch Life Sci, Shanghai 200444, Peoples R China
2.Chinese Acad Sci, Shanghai Inst Biol Sci, Inst Physiol, Grad Sch Chinese Acad Sci, Shanghai 200031, Peoples R China
3.Fudan Univ, Shanghai Med Coll, State Key Lab Med Neurobiol, Shanghai 200032, Peoples R China
Recommended Citation
GB/T 7714
Shi, Jian,He, Hui Qiong,Zhao, Rong,et al. Inhibition of martentoxin on neuronal BK channel subtype (alpha+beta 4): Implications for a novel interaction model[J]. BIOPHYSICAL JOURNAL,2008,94(9):3706-3713.
APA Shi, Jian.,He, Hui Qiong.,Zhao, Rong.,Duan, Yan-Hong.,Chen, Jin.,...&Ji, Yong Hua.(2008).Inhibition of martentoxin on neuronal BK channel subtype (alpha+beta 4): Implications for a novel interaction model.BIOPHYSICAL JOURNAL,94(9),3706-3713.
MLA Shi, Jian,et al."Inhibition of martentoxin on neuronal BK channel subtype (alpha+beta 4): Implications for a novel interaction model".BIOPHYSICAL JOURNAL 94.9(2008):3706-3713.
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