重组β2-肾上腺素能受体信号：利用非规范GRK功能治疗代谢性疾病

IF 52.7 1区医学 Q1 BIOCHEMISTRY & MOLECULAR BIOLOGY

Signal Transduction and Targeted Therapy Pub Date : 2025-09-12 DOI:10.1038/s41392-025-02407-4

Sean A. Cullum, Andreas Bock

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引用次数: 0

摘要

在最近发表在Cell上的一项研究中，Motso等人1开发了一系列G蛋白偶联受体激酶2 （GRK2）偏向β2-肾上腺素能受体（β2AR）的激动剂，这些激动剂显示出刺激肌肉葡萄糖摄取的功效，而不会引起与全身应用β-激动剂相关的心脏副作用2候选药物化合物15在1期临床试验中耐受性良好，可能为2型糖尿病和肥胖提供有希望的替代治疗选择

本文章由计算机程序翻译，如有差异，请以英文原文为准。

Rewiring β2-adrenergic receptor signaling: harnessing non-canonical GRK functions to treat metabolic diseases

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Rewiring β2-adrenergic receptor signaling: harnessing non-canonical GRK functions to treat metabolic diseases

In a study published recently in Cell, Motso et al.¹ developed a series of G protein-coupled receptor kinase 2 (GRK2)-biased agonists for the β₂-adrenergic receptor (β₂AR) which showed efficacy in stimulating muscular glucose uptake without eliciting cardiac side effects typically associated with systemically applied β-agonists.² The candidate drug, compound 15, was well-tolerated in a phase 1 clinical trial and could provide a promising alternative treatment option for type 2 diabetes and obesity.¹

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来源期刊

Signal Transduction and Targeted Therapy Biochemistry, Genetics and Molecular Biology-Genetics

CiteScore

44.50

自引率

1.50%

发文量

384

审稿时长

5 weeks

期刊介绍： Signal Transduction and Targeted Therapy is an open access journal that focuses on timely publication of cutting-edge discoveries and advancements in basic science and clinical research related to signal transduction and targeted therapy. Scope: The journal covers research on major human diseases, including, but not limited to: Cancer,Cardiovascular diseases,Autoimmune diseases,Nervous system diseases.