Summary
The white paper explores the immense therapeutic potential of G protein-coupled receptors (GPCRs), the largest family of membrane proteins in the human genome, comprising more than 800 members. GPCRs regulate diverse physiological processes, including sensory perception, immune responses, and cellular signaling. A key focus of this paper is GPCR drug discovery biased signaling, an emerging paradigm where ligands selectively stabilize specific receptor conformations to activate distinct pathways. This approach enables researchers to decouple therapeutic efficacy from adverse effects by targeting beneficial pathways while avoiding deleterious ones. New innovations are discussed that reshape GPCR-targeted drug discovery by unlocking previously inaccessible receptor targets and driving next-generation therapeutics with enhanced efficacy and safety profiles