GPCR dimerization: Drug discovery aspects and targets in renin-angiotensin systems

IF 2 Q3 BIOCHEMISTRY & MOLECULAR BIOLOGY FASEB bioAdvances Pub Date : 2025-01-31 DOI:10.1096/fba.2024-00180
Tahmid Faisal, Tahir Hussain
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Abstract

G protein-coupled receptors (GPCRs), which play crucial roles in various physiological functions, often assembled into dimers and higher-order oligomers. This oligomerization phenomenon has been observed in diverse physiological and pathological contexts, presenting promising opportunities for drug discovery targeting vital systems such as the cardiovascular, nervous, endocrine, and renal systems. This review offers a concise understanding of GPCR dimerization, its signaling mechanisms, and its implications. Furthermore, we explored therapeutic strategies aimed at modulating receptors involved in dimer/oligomer formation within the renin-angiotensin system.

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GPCR二聚化:肾素-血管紧张素系统中的药物发现方面和靶点
G蛋白偶联受体(gpcr)在各种生理功能中起着至关重要的作用,通常组装成二聚体和高阶低聚体。这种寡聚化现象已经在多种生理和病理环境中被观察到,为针对心血管、神经、内分泌和肾脏系统等重要系统的药物发现提供了有希望的机会。这篇综述提供了GPCR二聚化的简明理解,它的信号机制,及其意义。此外,我们探索了旨在调节肾素-血管紧张素系统中参与二聚体/低聚物形成的受体的治疗策略。
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来源期刊
FASEB bioAdvances
FASEB bioAdvances Multiple-
CiteScore
5.40
自引率
3.70%
发文量
56
审稿时长
10 weeks
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