Description
Book SynopsisIon channel drug discovery is a rapidly evolving field fuelled by recent, but significant, advances in our understanding of ion channel function combined with enabling technologies such as automated electrophysiology. The resurgent interest in this target class by both pharmaceutical and academic scientists was clearly highlighted by the over-subscribed RSC/BPS 'Ion Channels as Therapeutic Targets' symposium in February 2009. This book builds on the platform created by that meeting, covering themes including advances in screening technology, ion channel structure and modelling and up-to-date case histories of the discovery of modulators of a range of channels, both voltage-gated and non-voltage-gated channels. The editors have built an extensive network of contacts in the field through their first-hand scientific experience, collaborations and conference participation and the organisation of the meeting at Novartis, Horsham, increased the network enabling the editors to draw on the experience of eminent researchers in the field. Interest and investment in ion channel modulation in both industrial and academic settings continues to grow as new therapeutic opportunities are identified and realised for ion channel modulation. This book provides a reference text by covering a combination of recent advances in the field, from technological and medicinal chemistry perspectives, as well as providing an introduction to the new 'ion channel drug discoverer'. The book has contributions from highly respected academic researchers, industrial researchers at the cutting edge of drug discovery and experts in enabling technology. This combination provides a complete picture of the field of interest to a wide range of readers.
Table of ContentsPreface; Chanelling drug discovery; Chanome old and new; High throughput screening; Automated electrophysiology; Structure/crystallization/modeling studies; Toxins - does nature do ion channel drug discovery better than us? Structure and function of Sodium Channels, pharmacophores and binding sites; AMPA modulators - a case history; Inhibition of the epithelial sodium channel (ENaC) as a therapeutic approach to respiratory disease; CFTR channel modulation as a therapeutic approach; TRPs are a pain: a case history on TRPV1 antagonist development; The Retigabine story - the M current to therapeutically useful anticonvulsant; Icrac and Orai - a STIMulating channel; hERG past, present and future? Antibodies as ion channel modulators; Summary and the future; Index
