Assessing The Effects of Ligand-Binding Mutations to AMPA and Kainate Receptor Kinetics

When an agonist binds to the active site of a receptor channel, it interacts directly with a handful of key residues and indirectly with others to initiate a sequence of conformational steps that lead to channel opening. In the case of AMPA and KA receptors, they also lead to very rapid desensitization on a comparable time scale. Precisely which residues are most important to which processes, and how the receptor–ligand interactions impact various measures of channel function have yet to be fully elucidated. In this chapter I describe our approach to making single-point mutations in the ligand-binding domain and assessing the functional consequences of those mutations on critical measures of receptor-channel function.
Source: Springer protocols feed by Neuroscience - Category: Neuroscience Source Type: news