G-protein coupled receptors (GPCRs) are transmembrane proteins involved in a wide range of cell signalling processes. Their regulation through small molecule modulators is used for the treatment of different types of diseases and GPCRs currently account for more than 30% of drug targets. Recent evidence has highlighted the role of the pH-sensing GPR68 receptor in different cancers, so that it is considered as a new potential target in cancer therapy. The aim of this project is to understand the regulation mechanism of GPR68 and identify both selective antagonists and allosteric modulators using a combination of computational and experimental techniques.
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