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G protein-coupled receptors (GPCR) are seven transmembrane domains proteins involved in nearly all physiological processes. They compose the largest family of proteins in the human genome, with around 800 members. The most recent GRAFS classification identifies 5 main families: Glutamate, Rhodopsin, Adhesion, Frizzled and Secretin. The number and importance of physiological processes regulated by GPCRs is massive and has been investigated for decades. It is currently estimated that GPCRs constitute the direct or indirect target of 60% of all marketed medicines. However, only a portion of the 350 non-olfactory receptors are validated as drug targets. In addition, about 100 GPCRs remain devoid of known synthetic or endogenous ligands and labeled as orphan. Thus, it can be stated that the majority of GPCRs have an unknown or elusive function and are understudied. This situation can be explained by the paucity of pharmacological tools, and more specifically small molecules ligands. The absence of chemical probes able to modify a receptor function precludes our understanding of their biological role.