Abstract:Endothelin receptors (ETA and ETB) are class A GPCRs activated by vasoactive peptide endothelins, and are involved in blood pressure regulation. ETB-selective signaling induces vasorelaxation, and thus selective ETB agonists are expected to be utilized for improved anti-tumour drug delivery and neuroprotection. The effectiveness of a highly ETB-selective endothelin analogue, IRL1620, has been investigated in clinical trials. Here, we report the crystal structures of human ETB receptor in complex with ETB-selec… Show more
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