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Understanding class B GPCR agonist binding

  1. Sarah Crunkhorn
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Class B G-protein-coupled receptors (GPCRs), which include the glucagon-like peptide 1 receptor (GLP1R) and parathyroid hormone receptor 1 (PTH1R), are peptide hormone receptors that represent attractive therapeutic targets for many disorders. However, in contrast to class A GPCRs, few small-molecule agonists of class B GPCRs have been discovered. The identification of orally available small-molecule drugs to replace the injectable peptide drugs targeting these receptors is highly desired.

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Nature Reviews Drug Discovery 22, 787 (2023)

doi: https://doi.org/10.1038/d41573-023-00141-6

References

  1. Zhao, L.-H. et al. Conserved class B GPCR activation by a biased intracellular agonist. Nature https://doi.org/10.1038/s41586-023-06467-w (2023)

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