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Subcellular G-protein coupled receptor signaling hints at greater therapeutic selectivity

机译：亚细胞G蛋白偶联受体信号提示更高的治疗选择性

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摘要

G-protein coupled receptors (GPCRs) evolved as specialized sensors of the extracellular environment. Comprising the largest family of cell surface receptors, GPCRs are common therapeutic targets. Over the last 25 years, several GPCRs have been observed at the cell nucleus, suggesting the presence of intracrine GPCR signaling beyond the plasma membrane. Yet specific physiological functions of nuclear GPCRs had not been reported, until lately. We recently uncovered distinct but complementary angiogenic roles of F2rl1 (formerly known as PAR2) depending on its subcellular localization at the plasma membrane or at the nucleus. Targeting subcellular compartments to improve drug selectivity may therefore inspire novel therapeutic strategies for transmembrane receptors.
机译：G蛋白偶联受体（GPCR）演变为细胞外环境的专门传感器。 GPCR包含最大的细胞表面受体家族，是常见的治疗靶标。在过去的25年中，已经在细胞核上观察到了几种GPCR，这表明存在胞质内GPCR信号超出质膜。直到最近，尚未报道核GPCR的特定生理功能。我们最近发现F2rl1（以前称为PAR2）具有独特但互补的血管生成作用，这取决于它在质膜或细胞核上的亚细胞定位。因此，靶向亚细胞区室以改善药物选择性可以激发跨膜受体的新治疗策略。

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