SODIUM CHANNEL REGULATORS AND MODULATORS

摘要

The present invention provides a method of identifying a modulator of a voltage gated sodium channel (VGSC), which method comprises: (a) bringing into contact a test compound, a VGSC and one or more binding partners selected from PAPIN, periaxin and HSPC025 under conditions where the VGSC and the binding partner(s) are capable of forming a complex in the absence of the test compound; and (b) measuring an activity of the VGSC, wherein a change in the activity of the VGSC relative to the activity in the absence of the test compound indicates that the test compound is a modulator of said VGSC. Compounds identified in such screening methods are proposed for use in the treatment of VGSC-related conditions, for example in the treatment or prevention of pain. Also provided are methods of enhancing the functional expression of a voltage gated sodium channel (VGSC) in a cell comprising the step of increasing the level of a binding partner of the invention in the cell.