Biasing the odds: Approaches to capturing, understanding and exploiting functional selectivity in GPCRs

There is significant expectation in the pharmacological community that an understanding of biased signalling will lead to the development of new drugs and a better understanding of molecular targets in the in vivo context. I think it is safe to say that Pharma is withholding judgment on the promise and potential of what they view as an interesting pharmacological curiosity. That said, beyond successes of biased ligands in clinical trials and their appearance on the market, what it is need is a clear plan and the right tools and analytical methods to characterize functional selectivity from in cellulo to in vivo. In this issue of Methods, we have put together a series of articles that help lay out a methodological and analytical framework to help get us there.