Reichetzeder et al. "Head to Head Comparison of Structurally Unrelated DPP4 Inhibitors in the Setting of Renal Ischemia Reperfusion Injury" British Journal of Pharmacology (2017). Agonists acting at GPCRs promote biased signalling via Gα or Gβγ subunits, GPCR kinases and β‐arrestins. Since the demonstration of biased agonism has implications for drug discovery, it is essential to consider confounding factors contributing to bias. We have examined bias at human α1A‐adrenoceptors stably expressed at low levels in CHO‐K1 cells, identifying off‐target effects at endogenous receptors that contribute to ERK1/2 phosphorylation in response to the agonist oxymetazoline.
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