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Ion Channels - Articles and news items

Chloride ion channels and transporters

Chloride ion channels and transporters: from curiosities of nature and source of human disease to drug targets

Drug Targets, Issue 4 2013 / 20 August 2013 / Jonathan D. Lippiat, School of Biomedical Sciences, University of Leeds

Early in their undergraduate education, the student is introduced to various types of integral membrane protein: receptors, adhesion proteins, ion channels, ion pumps and ion transporters. As they progress through their studies, they find out that discrete gene families and protein structures are responsible for these different protein classes and there is never any reason to consider that there might be any ambiguity in assigning any particular protein to its appropriate protein class.

Figure 1 Cardiac safety schematic integrating indirect ion channel modulation analysis

Indirect modulation of cardiac ion channels and implications for preclinical safety assessment

Drug Targets, Issue 4 2010 / 19 August 2010 / Gül Erdemli & Dmitri Mikhailov, Center for Proteomic Chemistry, Novartis Institutes for BioMedical Sciences and Albert M Kim, Translational Medicine, Novartis Institutes for BioMedical Sciences

The preclinical assessment of a small molecule’s liability for QT interval prolongation is an essential part of the drug discovery process. Patch clamp assays for heterologously expressed recombinant cardiac ion channels are widely used in the pharmaceutical industry to evaluate potential drug-channel interactions. These assays are generally acute assessments and are not designed to detect indirect channel modulations that may result in QT prolongation. Despite the abundant literature demonstrating potential transcriptional, translational and post-translational mechanisms for indirect ion channel modulation, contribution of these mechanisms to drug-induced QT prolongation and/or arrhythmia propensity is not well understood. In this brief review, we discuss some potential mechanisms through which indirect ion channel modulation can produce QT prolongation and strategies for their early detection and mitigation.

 

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