GPCRs are valuable drug targets
GPCRs are a family of proteins that play an essential part in cell signalling and are thus important drug targets for modulating cell function and influencing disease outcome. The Class B subset of GPCRs includes many peptide hormone receptors relevant for treating disease, such as glucagon, glucagon-like peptide, calcitonin and parathyroid peptide hormone. However, until the recent work carried out by Heptares, it had proven almost impossible to provide structural data for this class, severely hampering drug development efforts across the industry.
The finding that the structure of CRF1, a Class B GPCR, contains a novel binding pocket for the small molecule antagonist, towards the intracellular side of the receptor and far from the position of other Class A GPCR ligands, underlines the importance of the discovery; particularly in terms of modelling other Class B receptors and potentially unlocking drug design across the subset.
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