There is increasing interest in developing FPR2 agonists (compound 43, ACT-389949 and BMS-986235) as potential pro-resolving therapeutics, with ACT-389949 and BMS-986235 having entered phase I clinical development. FPR2 activation leads to diverse downstream outputs. ACT-389949 was observed to cause rapid tachyphylaxis, while BMS-986235 and compound 43 induced cardioprotective effects in preclinical models. We aim to characterise the differences in ligand-receptor engagement and downstream signalling and trafficking bias profile.

中文翻译：

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结构不同的甲酰肽受体 2 激动剂的偏倚受体信号传导和细胞内运输谱


随着 ACT-389949 和 BMS-986235 进入 I 期临床开发，人们对开发 FPR2 激动剂（化合物 43、ACT-389949 和 BMS-986235）作为潜在的促消退疗法的兴趣越来越大。FPR2 激活导致不同的下游输出。观察到 ACT-389949 会引起快速耐受，而 BMS-986235 和化合物 43 在临床前模型中诱导心脏保护作用。我们旨在表征配体-受体参与以及下游信号传导和运输偏倚谱的差异。