A novel drug screening system
Drug screening can often be a laborious and time-consuming process involving the identification of molecular targets, and the isolation and subsequent testing of various compounds. An integrated approach whereby the experimental outcome could be predicted based on the target properties and the chemical structure of the compound would greatly facilitate and speed up the drug screening process. The key objective of the EU-funded ION project was to develop improved technical systems for testing chemical compounds which can act on ion channels and that might be used therapeutically. Partners addressed many aspects of this screening system, including the adaptation of emerging electrophysiology equipment and the development of intelligent software. An improved ion channel experimental platform (IONEP) was generated using a one-electrode system to measure changes in the current through ion channels in the membrane. The information regarding ion channels were integrated in an annotated ION Target Library which defined the most suitable ion channel targets for drug discovery in a given context of diseases. In a similar way, the ION Chemical Library was a prototype annotated collection of known chemical structures showing pharmacological activity. Based on the chemical structure in relation to a specific ion channel target, the ION Sequential Screening Software was designed to estimate in silico the pharmacological activity (IC50) of a given compound. The ION platform introduced two major innovations: easy access to a large set of targets and to an efficient drug discovery process. The exploitation of a library of starting molecular structures will facilitate the rapid analysis of data and aid the sequential design of future experiments, speeding up the entire process.
