It has become clear that GPCR can transduce signal using a much greater diversity of modalities than originally anticipated. Far from being linear communication lines, GPCR signaling pathways are more akin to web-like structures involving many different partners and mechanisms underlying the spatiotemporal propagation of diverse signals. In recent years, the concepts of biased-signaling and organelle-specific signaling are changing our vision of how the receptors and their signaling partners can be pharmacologically targeted for the development of better and safer drugs. The symposium will explore the multiple dimensions of GPCR signaling, the mechanisms controlling their selectivity and efficacy with a special focus on the possibility of harnessing this knowledge for the discovery of innovative therapies.