超越G蛋白和抑制蛋白：GRK2偏向性β₂肾上腺素能受体信号传导。
Beyond G protein and arrestin: GRK2-biased β₂AR signaling.
作者信息
Ji Ren-Lei, Wang Zhe, Zhao Jean J
机构信息
Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA 02215, USA; Department of Biological Chemistry and Molecular Pharmacology, Harvard Medical School, Boston, MA 02215, USA.
Department of Cancer Biology, Dana-Farber Cancer Institute, Boston, MA 02215, USA.
出版信息
Trends Pharmacol Sci. 2025 Aug 1. doi: 10.1016/j.tips.2025.07.010.
Abstract
Biased G-protein-coupled receptor (GPCR) signaling is reshaping drug discovery by enabling pathway-selective drug action. Recent work by Motso et al. identified GPCR kinase 2 (GRK2) as a non-canonical transducer, independent of G proteins or β-arrestins, redefining the biased signaling landscape and highlighting GRK2 as a novel therapeutic target for selective modulation of GPCR-driven metabolic responses.
摘要
偏向性G蛋白偶联受体（GPCR）信号传导通过实现途径选择性药物作用，正在重塑药物发现领域。Motso等人最近的研究确定GPCR激酶2（GRK2）是一种非经典转导分子，独立于G蛋白或β-抑制蛋白，重新定义了偏向性信号传导格局，并突出了GRK2作为选择性调节GPCR驱动的代谢反应的新型治疗靶点。
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