Conopeptide Vt3.1 Preferentially Inhibits BK Potassium Channels Containing β4 Subunits via Electrostatic Interactions

Li, Min; Chang, Shan; Yang, Longjin; Shi, Jingyi; McFarland, Kelli; Yang, Xiao; Moller, Alyssa; Wang, Chunguang; Zou, Xiaoqin; Chi, Cheng-Wu; Cui, Jianmin

doi:10.1074/jbc.m113.535898

Cited by 15 publications

(14 citation statements)

References 50 publications

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“…Alternatively, it is possible that β4 subunits control BK channel function through their ability to restrict plasma membrane localization of BK α tetramers (see Section 2.3); in this scenario, BK β4 may be highly expressed but retained within the endoplasmic reticulum and not present in plasma membrane BK channels (Shruti et al, 2012). Martentoxin and conopeptide Vt3.1 were reported to preferentially inhibit β4-containing BK channels and could help provide novel insights into this question, but, as for iberiotoxin, the ratio of β4 subunits required to drive increased sensitivity to these inhibitors remains to be determined (Li, Chang, et al, 2014; Shi et al, 2008). …”

Section: Expression Patterns Of Bk Channel Subunits In the Cnsmentioning

confidence: 99%

BK Channels in the Central Nervous System

Contet

Goulding

Kuljis

et al. 2016

International Review of Neurobiology

135

170

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Large conductance Ca2+- and voltage-activated K+ (BK) channels are widely distributed in the postnatal central nervous system (CNS). BK channels play a pleiotropic role in regulating the activity of brain and spinal cord neural circuits by providing a negative feedback mechanism for local increases in intracellular Ca2+ concentrations. In neurons, they regulate the timing and duration of K+ influx such that they can either increase or decrease firing depending on the cellular context, and they can suppress neurotransmitter release from presynaptic terminals. In addition, BK channels located in astrocytes and arterial myocytes modulate cerebral blood flow. Not surprisingly, both loss and gain of BK channel function have been associated with CNS disorders such as epilepsy, ataxia, mental retardation, and chronic pain. On the other hand, the neuroprotective role played by BK channels in a number of pathological situations could potentially be leveraged to correct neurological dysfunction.

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Section: Expression Patterns Of Bk Channel Subunits In the Cnsmentioning

confidence: 99%

BK Channels in the Central Nervous System

Contet

Goulding

Kuljis

et al. 2016

International Review of Neurobiology

135

170

View full text Add to dashboard Cite

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“…But the binding between slotoxin and the BKα/β4 channel seemed to be irreversible in an unknown mechanism (Garcia-Valdes, Zamudio, Toro, & Possani, 2001). In contrast, martentoxin (Shi et al, 2008; Tao, Shi, Liu, & Ji, 2012) and conopeptide Vt3.1 (Li et al, 2014) were identified as the more selective blockers for the BKα/β4 channel, but not BKα/β1 channel, when compared with BKα channel alone. The β subunits were also reported to regulate BK channel modulation by ethanol.…”

Section: Modulation Of the Bk Channel's Pharmacological Propertiesmentioning

confidence: 99%

Modulation of BK Channel Function by Auxiliary Beta and Gamma Subunits

Yan

2016

International Review of Neurobiology

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The large-conductance, Ca2+- and voltage-activated K+ (BK) channel is ubiquitously expressed in mammalian tissues and displays diverse biophysical or pharmacological characteristics. This diversity is in part conferred by channel modulation with different regulatory auxiliary subunits. To date, two distinct classes of BK channel auxiliary subunits have been identified: β subunits and γ subunits. Modulation of BK channels by the four auxiliary β (β1–β4) subunits has been well established and intensively investigated over the past two decades. The auxiliary γ subunits, however, were identified only very recently, which adds a new dimension to BK channel regulation and improves our understanding of the physiological functions of BK channels in various tissues and cell types. This chapter will review the current understanding of BK channel modulation by auxiliary β and γ subunits, especially the latest findings.

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“…So crude extracts of these toxins can be safely used in animal models. The conopeptide Vt3.1 preferentially inhibited the BK channels containing the α + β4 subunits [87]. …”

Section: Bkβ (Kcnmb) Chainsmentioning

confidence: 99%

Big Potassium (BK) ion channels in biology, disease and possible targets for cancer immunotherapy

Hoa

Wilson

et al. 2014

International Immunopharmacology

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The Big Potassium (BK) ion channel is commonly known by a variety of names (Maxi-K, KCNMA1, slo, Stretch-activated potassium channels, KCa1.1). Each name reflects a different physical property displayed by this single ion channel. This transmembrane channel is found on nearly every cell type of the body and has its own distinctive roles for that tissue type. The BKα channel contains the pore that releases potassium ions from intracellular stores. This ion channel is found on the cell membrane, endoplasmic reticulum, Golgi and mitochondria. Complex splicing pathways produce different isoforms. The BKα channels can be phosphorylated, palmitoylated and myristylated. BK is composed of a homo-tetramer that interacts with β and γ chains. These accessory proteins provide a further modulating effect on the functions of BKα channels. BK channels play important roles in cell division and migration. In this review, we will focus on the biology of BK channels, especially its role, and that it has in the immune response towards cancer. Recent proteomic studies have linked BK channels with various proteins. Some of these interactions offer further insight into the role that BK channels have with cancers, especially with brain tumors. This review shows that BK channels have a complex interplay with intracellular components of cancer cells and still have plenty of secrets to be discovered.

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Conopeptide Vt3.1 Preferentially Inhibits BK Potassium Channels Containing β4 Subunits via Electrostatic Interactions

Cited by 15 publications

References 50 publications

BK Channels in the Central Nervous System

BK Channels in the Central Nervous System

Modulation of BK Channel Function by Auxiliary Beta and Gamma Subunits

Big Potassium (BK) ion channels in biology, disease and possible targets for cancer immunotherapy

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