G-Protein Coupled Receptors

It has always been popular to start companies around families and subfamilies of targets, banking on the similarity among the receptors to speed drug discovery. But the idea largely hasn't panned out, in part because of the new target risk--sometimes they're not pharmaceutically relevant and sometimes they resist the available chemistries. That's why G-protein coupled receptors (GPCRs) have been so important: they're clearly relevant (many, perhaps most, blockbusters come from this class of receptor) and their unique structure makes them both relatively easy to hit with ligands and likely to do something when hit. But the same structural advantages turn into scientific disadvantages for researchers: they resist screening and other techniques of modern drug discovery. We explore some of the newest approaches to mining this rich vein of opportunity.