Inhibition of martentoxin on neuronal BK channel subtype (alpha+beta 4): Implications for a novel interaction model

IMR OpenIR

	Inhibition of martentoxin on neuronal BK channel subtype (alpha+beta 4): Implications for a novel interaction model
	Shi, Jian 2; He, Hui Qiong 2; Zhao, Rong 2; Duan, Yan-Hong 1; Chen, Jin 2; Chen, Ying 1; Yang, Juan 1; Zhang, Jian Wei 1; Shu, Xue Qin 1; Zheng, Ping 3; Ji, Yong Hua 1
通讯作者	Ji, Yong Hua(yhji@staff.shu.edu.cn)
	2008-05-01
发表期刊	BIOPHYSICAL JOURNAL
ISSN	0006-3495
卷号	94 期号:9 页码:3706-3713
摘要	Martentoxin 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.
收录类别	SCI
语种	英语
WOS研究方向	Biophysics
WOS类目	Biophysics
WOS记录号	WOS:000254829700031
出版者	BIOPHYSICAL SOC
引用统计	被引频次：27[WOS] [WOS记录] [WOS相关记录]
文献类型	期刊论文
条目标识符	http://ir.imr.ac.cn/handle/321006/93369
专题	中国科学院金属研究所
通讯作者	Ji, Yong Hua
作者单位	1.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
推荐引用方式 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.