Contributions of the membrane dipole potential to the function of voltage-gated cation channels and modulation by small molecule potentiators

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• 作者：Robert A. Pearlstein ; ^{robert.pearlstein@novartis.com} ; Callum J. Dickson ; Viktor Hornak
• 关键词：MD ; Molecular dynamics ; QM ; quantum mechanics ; human Ether-a-go-go-Related Gene ; hERG ; VS ; voltage-sensing domain
• 刊名：Biochimica et Biophysica Acta (BBA) - Biomembranes
• 出版年：2017
• 出版时间：February 2017
• 年：2017
• 卷：1859
• 期：2
• 页码：177-194
• 全文大小：3685 K
• 卷排序：1859

文摘

The transmembrane potential and dipole potential serve as barriers to voltage-gated ion channel activation and deactivation. Modulation of the dipole potential by small molecules may alter the rates of activation and deactivation. Dipole potential lowering by a series of positive hERG potentiators is strongly correlated with the degree of potentiation.