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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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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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Ion-exchange chromatography, or IEC, is a technique for separating ions based on their affinity for the stationary phase. The stationary phase is a cross-linked polymer resin with covalently attached ionic functional groups. The functional groups can be either positively charged (cation exchangers) or negatively charged (anion exchangers). A cation exchanger consists of a polymeric anion and active cations, while an anion exchanger is a polymeric cation with active anions. The choice of...
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Updated: Feb 17, 2026

Author Spotlight: Exploring the Role of Ion Channels in Cancer: Characterization and Potential Treatment Approaches
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Assay technologies for screening ion channel targets.

L C Mattheakis1, A Savchenko

  • 1Affymax Research Institute, 4001 Miranda Ave, Palo Alto, CA 94304, USA. lmattheakis@qdots.com

Current Opinion in Drug Discovery & Development
|December 1, 2001
PubMed
Summary

Developing reliable high-throughput screening (HTS) assays is crucial for discovering drugs targeting new ion channel genes. Cell-based functional assays are preferred for sensing ion channel states in drug discovery programs.

Area of Science:

  • Pharmacology
  • Molecular Biology
  • Genomics

Background:

  • The human genome sequencing is identifying numerous novel ion channel genes.
  • Ion channels are critical drug targets, particularly for diseases.
  • Existing drug discovery methods need adaptation for these new targets.

Purpose of the Study:

  • To review and evaluate cell-based assays for high-throughput screening (HTS) of ion channels.
  • To discuss the importance of functional assays for dynamic ion channel proteins.
  • To explore future directions for improving ion channel assay development.

Main Methods:

  • Review of existing literature on cell-based functional assays for ion channels.
  • Comparison of cell-based assays with traditional competition-binding assays.

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  • Analysis of assay requirements for sensing various ion channel functional states.

    • Main Results:

    • Competition-binding assays are often insufficient for ion channel drug discovery.
    • Cell-based functional assays are more suitable for HTS of ion channels.
    • Assays must be robust and reliable to identify modulators of specific ion channel functions.

    Conclusions:

    • Cell-based functional assays are essential for effective ion channel drug discovery.
    • Further improvements in assay technology are needed to fully exploit new ion channel targets.
    • Reliable HTS assays are key to developing drugs for ion channel-related diseases.