Simple Summary Therapy for nonfunctioning pituitary adenomas (NFPAs) is a significant unmet medical need since these adenomas are frequently invasive, are difficult to resect completely and often recur. NFPAs express high levels of somatostatin receptor 3 (SSTR3), and SSTR3 agonists could be a promising…
Abstract Analysis of agonist-driven phosphorylation of G protein-coupled receptors (GPCRs) can provide valuable insights into the receptor activation state and ligand pharmacology. However, to date, assessment of GPCR phosphorylation using high-throughput applications has been challenging. We have developed…
In addition to the classical oestrogen receptors, ERα and ERβ, a G protein-coupled oestrogen receptor (GPER) has been identified that primarily mediates the rapid, non-genomic signalling of oestrogens. Data on GPER expression at the protein level are contradictory; therefore, the present study was conducted…
Multi-receptor targeting has been proposed as a promising strategy for the development of opioid analgesics with fewer side effects. Cebranopadol and AT-121 are prototypical bifunctional ligands targeting the nociceptin/orphanin FQ peptide receptor (NOP) and µ-opioid receptor (MOP) that elicit potent…
London: Macmillan Publishers Limited, part of Springer Nature, 2022-05-03