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Ion channel drug discovery: challenges and future directions
A Wickenden1, B Priest, G Erdemli
1Johnson & Johnson Pharmaceutical Research & Development, L.L.C., 3210 Merryfield Row, San Diego, CA 92121, USA.
Future Medicinal Chemistry
|March 31, 2012
Summary
Ion channel drug discovery faces challenges due to assay limitations, despite significant market value. Advances in automated electrophysiology and novel approaches may unlock the therapeutic potential of over 400 ion channel targets.
Area of Science:
- Pharmacology
- Neuroscience
- Biotechnology
Background:
- Ion channels are crucial drug targets, with current drug sales reaching approximately US$12 billion.
- Over 400 ion channel genes are known, yet they remain largely under-exploited therapeutic targets.
- Limitations in high-throughput assay technologies hinder effective screening and lead optimization for ion channel drug discovery.
Purpose of the Study:
- To review the current status of ion channel drug discovery.
- To discuss the major challenges and limitations in the field.
- To propose alternative strategies for future ion channel drug development.
Main Methods:
- Review of existing literature on ion channel drug discovery.
- Analysis of current high-throughput screening technologies, including automated electrophysiology.
- Discussion of challenges and potential solutions in the field.
Main Results:
- Automated electrophysiology shows promise for improving screening efficiency.
- Significant limitations persist in current assay technologies.
- Over 400 ion channel targets offer vast, yet untapped, therapeutic potential.
Conclusions:
- Despite market success, ion channel drug discovery is hampered by technological limitations.
- Automated electrophysiology and innovative approaches are crucial for overcoming these hurdles.
- Future research should focus on developing advanced assays to fully exploit ion channels as therapeutic targets.
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