Chemical-biology approaches to pathway selective adenosine receptor ligands

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This project aims to develop new chemical-biology tools and approaches for selectively targeting signalling pathways mediated by G protein-coupled receptors (GPCR). GPCRs are an important family of cell surface signalling proteins that are responsible for the regulation of numerous vital physiological functions. The A1 adenosine receptor is an important model and therapeutically relevant GPCR that will be the focus of this project. Compounds known as bitopic ligands, which can interact with distinct binding sites (termed orthosteric and allosteric sites), will be explored as pathway selective agents capable of activating the signalling pathways mediating the desired effect in preference to those producing adverse effects. Longer-term benefits include the identification of bioactive compounds with more selective modes of action and improved safety profiles.