Chapters authored
Voltage-Gated Sodium Channels in Drug Discovery
Voltage-gated sodium channels (Nav) control the initiation and propagation of action potential, and thus mediate a broad spectrum of physiological processes, including central and peripheral nervous systems’ function, skeletal muscle contraction, and heart rhythm. Recent advances in elucidating the molecular basis of channelopathies implicating Nav channels are the most appealing druggable targets for pain and many other pathology conditions. This chapter overviews Nav super family from genetic evolution, distribution, human diseases/pathology association, highlighting the most recent structure function breakthrough. The second section will discuss current small and large Nav modulators, including traditional nonselective pore blockers, intracellular modulators, and extracellular modulators.
Part of the book: Ion Channels in Health and Sickness
Voltage-Gated Sodium Channel Drug Discovery Technologies and Challenges
Voltage-gated sodium (Nav) channels represent an important class of drug target for pain and many other pathology conditions. Despite the recent advances in channelopathies and structure-function studies, the discovery of Nav channel therapeutics is still facing a major challenge from the limitation of assay technologies. This chapter will focus on advancement and challenge of Nav drug discovery technologies including nonelectrophysiological assays, extracellular electrophysiological assays, and the newly evolved high-throughput automated patch clamp (APC) technologies.
Part of the book: Ion Channels in Health and Sickness