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Ion channels are important drug targets for a range of diseases including pain, epilepsy and addiction. However, progress towards the development of more selective inhibitors that generate fewer dose-limiting side effects, or open up new therapeutic opportunities, has been slow. Due to the potentially higher selectivity offered by venom peptides, many pharmaceutical companies are embracing biological-based approaches to the identification of novel ion channel modulators. This will help overcome some of the limitations of low molecular weight modulators, whose affinity is often driven by factors such as lipid solubility and interactions with more conserved transmembrane domains. This chapter will cover this rapidly emerging field, providing examples of venom peptide and small molecule approaches towards the development of Cav2.2, Nav1.7 and Kv1.3 inhibitors for the treatment of pain and autoimmune diseases.

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