The structure, function, and pharmacology of MRGPRs

被引：27

作者：

Cao, Can ^{[1
]}

Roth, Bryan L. ^{[1
,2
]}

机构：

[1] Univ N Carolina, Dept Pharmacol, Sch Med, Chapel Hill, NC 27599 USA

[2] Univ N Carolina, Eschelman Sch Pharm, NIMH Psychoact Drug Screening Program, Div Chem Biol & Med Chem, Chapel Hill, NC 27599 USA

来源：

TRENDS IN PHARMACOLOGICAL SCIENCES | 2023年 / 44卷 / 04期

基金：

美国国家卫生研究院;

关键词：

PROTEIN-COUPLED RECEPTOR; MAST-CELLS; GENE X2; ITCH; ACTIVATION; DISCOVERY; EXCITABILITY; SODIUM; MODELS; SKIN;

D O I：

10.1016/j.tips.2023.02.002

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

Mas-related G protein-coupled receptor (MRGPR) family members play important roles in the sensation of noxious stimuli and represent novel targets for the treatment of itch and pain. MRGPRs recognize a diversity of agonists and display complicated downstream signaling profiles, high sequence diversity across species, and many polymorphisms in humans. The recent structural advances on MRGPRs reveal unique structural features and diverse agonist recognition modes of this receptor family, which should facilitate the structure-based drug discovery at MRGPRs. In addition, the newly discovered ligands also provide valuable tools to explore the function and the therapeutic potential of MRGPRs. In this review, we discuss these progresses in our understanding of MRGPRs and highlight the challenges and potential opportunities for the future drug discovery at these receptors.

引用

页码：237 / 251

页数：15

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