Decursin from Angelica gigas Nakai Blocks hKv1.5 Channel

Kwak, Yong-Geun; Choi, Byoung Han; Kim, Daekeun; Eun, Jae-Soon

doi:10.4062/biomolther.2011.19.1.033

Biomolecules and Therapeutics

2011

DOI: 10.4062/biomolther.2011.19.1.033

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Decursin from Angelica gigas Nakai Blocks hKv1.5 Channel

Yong-Geun Kwak¹,

Byoung Han Choi²,

Daekeun Kim³

et al.

Abstract: Kim et al., 2010). Our studies have focused on the development of antiarrhythmic drug, and we previously reported that papaverine (Choe et al., 2003), oxypeucedanin (Eun et al., 2005b), psoralen and their derivatives (Eun at al., 2005a;Eun et al., 2007) and torilin (Kwak et al., 2006) inhibited the hKv1.5 current. The present study was examined to investigate the effect of decursin from A. gigas on hKv1.5 channels using the whole-cell patch-clamp technique.

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Challenges Faced with Small Molecular Modulators of Potassium Current Channel Isoform Kv1.5

Zhao

Ruan

et al. 2019

Biomolecules

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The voltage-gated potassium channel Kv1.5, which mediates the cardiac ultra-rapid delayed-rectifier (IKur) current in human cells, has a crucial role in atrial fibrillation. Therefore, the design of selective Kv1.5 modulators is essential for the treatment of pathophysiological conditions involving Kv1.5 activity. This review summarizes the progress of molecular structures and the functionality of different types of Kv1.5 modulators, with a focus on clinical cardiovascular drugs and a number of active natural products, through a summarization of 96 compounds currently widely used. Furthermore, we also discuss the contributions of Kv1.5 and the regulation of the structure-activity relationship (SAR) of synthetic Kv1.5 inhibitors in human pathophysiology. SAR analysis is regarded as a useful strategy in structural elucidation, as it relates to the characteristics that improve compounds targeting Kv1.5. Herein, we present previous studies regarding the structural, pharmacological, and SAR information of the Kv1.5 modulator, through which we can assist in identifying and designing potent and specific Kv1.5 inhibitors in the treatment of diseases involving Kv1.5 activity.

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Challenges Faced with Small Molecular Modulators of Potassium Current Channel Isoform Kv1.5

Zhao

Ruan

et al. 2019

Biomolecules

View full text Add to dashboard Cite

show abstract

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Decursin from Angelica gigas Nakai Blocks hKv1.5 Channel

Cited by 1 publication

References 15 publications

Challenges Faced with Small Molecular Modulators of Potassium Current Channel Isoform Kv1.5

Challenges Faced with Small Molecular Modulators of Potassium Current Channel Isoform Kv1.5

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