Kv1.3 channel as a promising therapeutic target for acquired aplastic anemia

Hu, Xiaojing; Xu, Cheng-Hui; Cong, Yaqin

doi:10.1016/j.mehy.2007.11.005

Cited by 2 publications

(2 citation statements)

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“…The PKC family comprises at least 12 serine/threonine kinase isozymes and is responsible for transducing many cellular signals that regulate the activity of different plasma membrane proteins, including ion channels (18,30). The ability of REV to activate or inhibit PKC activity is dependent on cell types.…”

Section: Discussionmentioning

confidence: 99%

Resveratrol inhibits K_v2.2 currents through the estrogen receptor GPR30-mediated PKC pathway

Dong

Chen

et al. 2013

American Journal of Physiology-Cell Physiology

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Resveratrol (REV) is a naturally occurring phytoalexin that inhibits neuronal K⁺ channels; however, the molecular mechanisms behind the effects of REV and the relevant α-subunit are not well defined. With the use of patch-clamp technique, cultured cerebellar granule cells, and HEK-293 cells transfected with the K(v)2.1 and K(v)2.2 α-subunits, we investigated the effect of REV on K(v)2.1 and K(v)2.2 α-subunits. Our data demonstrated that REV significantly suppressed Kv2.2 but not Kv2.1 currents with a fast, reversible, and mildly concentration-dependent manner and shifted the activation or inactivation curve of Kv2.2 channels. Activating or inhibiting the cAMP/PKA pathway did not abolish the inhibition of K(v)2.2 current by REV. In contrast, activation of PKC with phorbol 12-myristate 13-acetate mimicked the inhibitory effect of REV on K(v)2.2 by modifying the activation or inactivation properties of Kv2.2 channels and eliminated any further inhibition by REV. PKC and PKC-α inhibitor completely eliminated the REV-induced inhibition of K(v)2.2. Moreover, the effect of REV on K(v)2.2 was reduced by preincubation with antagonists of GPR30 receptor and shRNA for GPR30 receptor. Western blotting results indicated that the levels of PKC-α and PKC-β were significantly increased in response to REV application. Our data reveal, for the first time, that REV inhibited K(v)2.2 currents through PKC-dependent pathways and a nongenomic action of the oestrogen receptor GPR30.

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Section: Discussionmentioning

confidence: 99%

Resveratrol inhibits K_v2.2 currents through the estrogen receptor GPR30-mediated PKC pathway

Dong

Chen

et al. 2013

American Journal of Physiology-Cell Physiology

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“…The role of Kv1.3 in insulin sensitivity is summarized in Figure 1. Although Kv channel blockers are currently used for several diseases, recent studies have spotlighted Kv1.3 as a potential therapeutic target for treatment of autoimmune disease, type 2 diabetes, asthma, aplastic anemia and periodontal disease [24][25][26][27][28] .…”

Section: Kv13 In Insulin Sensitivitymentioning

confidence: 99%

Kv1.3: a potential pharmacological target for diabetes

Choi

Hahn

2010

Acta Pharmacol Sin

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K+ channels, which are ubiquitous membrane proteins, play a central role in regulating the resting membrane potential and the shape and duration of the action potential in pancreatic β-cells. There are at least three types of K + channels (K ATP , K Ca , and Kv2.1 channels) that are involved in glucose-stimulated insulin secretion in pancreatic β-cells, and one type (Kv1.3) that is associated with the regulation of insulin sensitivity in peripheral target tissues. This article reviews the function of Kv1.3 channels that contribute to mediating insulin action in insulin-sensitive tissues. Pharmacological strategies for targeting Kv1.3 are then discussed with a focus on a rationale for the potential therapeutic use of Kv1.3 blocker in diabetic treatment.

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Kv1.3 channel as a promising therapeutic target for acquired aplastic anemia

Cited by 2 publications

References 5 publications

Resveratrol inhibits K_v2.2 currents through the estrogen receptor GPR30-mediated PKC pathway

Resveratrol inhibits K_v2.2 currents through the estrogen receptor GPR30-mediated PKC pathway

Kv1.3: a potential pharmacological target for diabetes

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Kv1.3 channel as a promising therapeutic target for acquired aplastic anemia

Cited by 2 publications

References 5 publications

Resveratrol inhibits Kv2.2 currents through the estrogen receptor GPR30-mediated PKC pathway

Resveratrol inhibits Kv2.2 currents through the estrogen receptor GPR30-mediated PKC pathway

Kv1.3: a potential pharmacological target for diabetes

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Resveratrol inhibits K_v2.2 currents through the estrogen receptor GPR30-mediated PKC pathway

Resveratrol inhibits K_v2.2 currents through the estrogen receptor GPR30-mediated PKC pathway