TECHNOLOGY - Membrane proteins in Drug Discovery

Membrane proteins such as receptors and ion channels are key regulators of cellular function. Membrane proteins account for up to two thirds of known drugable targets, highlighting their critical pharmaceutical importance. The G protein-coupled receptors (GPCRs) are the largest, most versatile, group of membrane receptors and also the most pharmaceutically important, accounting for over 50% of all human drug targets and acting as therapeutic targets for a wide range of disease conditions including cancer, cardiovascular, metabolic, CNS and inflammatory diseases.

Ion channels represent another group of important membrane protein drug targets and account for for the activity of 10% of the currently marketed drugs: Despite their importance, membrane receptors are notoriously difficult to prepare in pure, correctly-folded form in sufficient quantity for drug discovery purposes. The M-FOLD™ platform was designed specifically to address issues associated with the discovery of therapeutics for low abundance membrane proteins, and primarily GPCRs and ion channels.

Drug target classes of current drug therapies

Reproduced from: J Drews, Science, Vol 287, p1960-1964 (2000)