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Related Concept Videos

Patch Clamp01:18

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Many fundamental cell functions such as muscle contraction and nerve transmission rely on the electrical signals produced by the movement of positively and negatively charged ions across the cell membrane. One competent method to record current flowing across the whole cell or single ion channel is the patch-clamp technique.
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Genetic screens are tools used to identify genes and mutations responsible for phenotypes of interest. Genetic screens help identify individuals or a group of people at risk of developing  genetic diseases and help them with early intervention, targeted therapy, and reproductive options.
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The movement of ions like sodium, potassium, and calcium into and out of the cell is essential to maintain the electrochemical gradient in living cells. The ion channels—a class of membrane transport proteins—help maintain this ionic gradient for the smooth functioning of physiological activities such as maintaining cell size and volume, conducting nerve impulses, and gas and nutrient exchange.
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High-throughput Screening for Small-molecule Modulators of Inward Rectifier Potassium Channels
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High throughput screening technologies for ion channels.

Hai-bo Yu1, Min Li1, Wei-ping Wang1

  • 1State Key Laboratory of Bioactive Substances and Functions of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China.

Acta Pharmacologica Sinica
|December 15, 2015
PubMed
Summary
This summary is machine-generated.

High throughput screening (HTS) assays for ion channels are crucial for drug discovery and understanding disease. This review covers the evolution and current applications of various HTS technologies for ion channel research.

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Area of Science:

  • Biochemistry
  • Pharmacology
  • Physiology

Background:

  • Ion channels are vital for physiological processes.
  • Dysfunctional ion channels are implicated in numerous human diseases.
  • Ion channels are key targets for drug development and off-target profiling.

Purpose of the Study:

  • To review current high throughput screening (HTS) technologies for ion channels.
  • To discuss the applications of these HTS methods across different ion channel classes.

Main Methods:

  • Chronological overview of HTS assay development for ion channels.
  • Discussion of ligand binding assays, flux-based assays, fluorescence-based assays, and automated electrophysiology.
  • Summary of advancements in functional assays and instrumentation.

Main Results:

  • Significant progress in developing and applying HTS for diverse ion channel types.
  • Established methodologies enable large-scale pharmacological profiling.
  • Technological advancements have expanded the scope of ion channel screening.

Conclusions:

  • HTS technologies are indispensable tools in ion channel research and drug discovery.
  • The evolution of assays has improved efficiency and scope in identifying channel modulators.
  • Continued innovation in HTS will further advance our understanding of ion channel function and disease.