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Update on Angiotensin II Subtype 2 Receptor: Focus on Peptide and Nonpeptide Agonists
Molecular Pharmacology ( IF 3.6 ) Pub Date : 2021-06-01 , DOI: 10.1124/molpharm.121.000236
Arina Ranjit 1 , Sana Khajehpour 1 , Ali Aghazadeh-Habashi 2
Affiliation  

Angiotensin II (Ang II) is the most dominant effector component of the renin-angiotensin system (RAS) that generally acts through binding to two main classes of G protein–coupled receptors, namely Ang II subtype 1 receptor (AT1R) and angiotensin II subtype 2 receptor (AT2R). Despite some controversial reports, the activation of AT2R generally antagonizes the effects of Ang II binding on AT1R. Studying AT2R signaling, function, and its specific ligands in cell culture or animal studies has confirmed its beneficial effects throughout the body. These characteristics classify AT2R as part of the protective arm of the RAS that, along with functions of Ang (1–7) through Mas receptor signaling, modulates the harmful effects of Ang II on AT1R in the activated classic arm of the RAS. Although Ang II is the primary ligand for AT2R, we have summarized other natural or synthetic peptide and nonpeptide agonists with critical evaluation of their structure, mechanism of action, and biologic activity.

中文翻译:

血管紧张素 II 亚型 2 受体更新:专注于肽和非肽激动剂

血管紧张素 II (Ang II) 是肾素-血管紧张素系统 (RAS) 中最主要的效应成分,通常通过与两大类 G 蛋白偶联受体结合起作用,即血管紧张素 II 亚型 1 受体 (AT1R) 和血管紧张素 II 亚型2 受体 (AT2R)。尽管有一些有争议的报道,但 AT2R 的激活通常会拮抗 Ang II 结合对 AT1R 的影响。在细胞培养或动物研究中研究 AT2R 信号传导、功能及其特定配体已证实其对全身的有益影响。这些特征将 AT2R 归类为 RAS 保护臂的一部分,与 Ang (1-7) 通过 Mas 受体信号传导的功能一起,调节 Ang II 对 RAS 激活的经典臂中 AT1R 的有害影响。虽然 Ang II 是 AT2R 的主要配体,
更新日期:2021-06-07
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