Abstract
Ion-channel protein complexes represent a promising and exciting class of therapeutic targets with applications across many disease indications. Drugs that modulate ion-channel activity are first-line therapies in several therapeutic areas, such as cardiovascular disorders, central and peripheral nervous system disorders, and metabolic disorders, and the use of specific ion-channel modulators will likely expand into other major therapeutic areas, such as oncology. However, the pharmaceutical and biotechnology industries have not aggressively exploited ion channels as drug targets because they require difficult, labor-intensive, and low-throughput assays. Fortunately, recent scientific and technological advances are affecting ion-channel R&D significantly. In this report, we examine the function of ion channels and potential ion-channel targets, describe traditional and new methods of screening, profile companies specializing in ion-channel research, and discuss the outlook for the field.
Table of Contents
Introduction
Ion-Channel Overview
- Function and Classification
- Many Potential Targets
- Undesirable Targets and HERG
- Few Marketed Ion-Channel Modulators
Screening Assays for the Discovery of Ion-Channel Modulators
- Traditional Screening Methods
- The Road to Higher Throughput
- New Screening Technologies
- Improved Fluorescent Assays
- High-Throughput Patch Clamping
- In Silico Methods
The Role of Specialist Companies
Corporate Highlights
- Icagen
- Lectus Therapeutics
- Neurion Pharmaceuticals
- Neuromed
- NeuroSearch
- Xention Discovery
Outlook for the Discovery of Ion-Channel Modulators
