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Factors influencing biased agonism in recombinant cells expressing the human α1A -adrenoceptor.

Edilson Dantas da Silva JuniorMasaaki SatoJon MerlinNatalie BroxtonDana S HutchinsonSabatino VenturaBronwyn A EvansRoger J Summers
Published in: British journal of pharmacology (2017)
We have shown that while adrenergic agonists display bias at human α1A -adrenoceptors, the marked bias of oxymetazoline for ERK1/2 phosphorylation originates from off-target effects. Commonly used cell lines express a repertoire of endogenous GPCRs that may confound studies on biased agonism at recombinant receptors.
Keyphrases
  • endothelial cells
  • induced pluripotent stem cells
  • induced apoptosis
  • pluripotent stem cells
  • signaling pathway
  • cell proliferation
  • oxidative stress
  • cell death
  • endoplasmic reticulum stress