CHAPTER 4: Structural Understanding of Ion Channels in Atomic Detail
Published:03 Sep 2014
Special Collection: 2014 ebook collection , 2011-2015 industrial and pharmaceutical chemistry subject collectionSeries: Drug Discovery
The first ion channel crystal structure was resolved nearly 15 years ago, in 1998, an achievement acknowledged by the award of the Nobel Prize for Chemistry to Rod MacKinnon, in 2003. Although these proteins remain difficult to crystallise there are an increasing number of structures available. This chapter discusses the history of the field, outlines some of the recent structural successes and describes the development of novel methods that have rendered ion channels, and membrane proteins in general, more tractable to structural biology. The wealth of information provided by all these structures enhances our understanding of channel structure and by inference allows us to understand their functional influence on the associated physiological processes. While many of the ion channel structures are bacterial in nature, recent developments have led to the structural elucidation of eukaryotic proteins that should facilitate future ion channel drug discovery.