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The Other Angiotensin II Receptor: AT2R as a Therapeutic Target.
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2020-02-07 , DOI: 10.1021/acs.jmedchem.9b01780
Lucienne Juillerat-Jeanneret 1
Affiliation  

The active hormone of the renin-angiotensin system (RAS), angiotensin II (Ang II), is involved in several human diseases, driving the development and clinical use of several therapeutic drugs, mostly angiotensin I converting enzyme (ACE) inhibitors and angiotensin receptor type I (AT1R) antagonists. However, angiotensin peptides can also bind to receptors different from AT1R, in particular, angiotensin receptor type II (AT2R), resulting in biological and physiological effects different, and sometimes antagonistic, of their binding to AT1R. In the present Perspective, the components of the RAS and the therapeutic tools developed to control it will be reviewed. In particular, the characteristics of AT2R and tools to modulate its functions will be discussed. Agonists or antagonists to AT2R are potential therapeutics in cardiovascular diseases, for agonists, and in the control of pain, for antagonists, respectively. However, controlling their binding properties and their targeting to the target tissues must be optimized.

中文翻译:

其他血管紧张素II受体:AT2R作为治疗靶标。

肾素-血管紧张素系统(RAS)的活性激素血管紧张素II(Ang II)参与多种人类疾病,推动了几种治疗药物的开发和临床使用,其中大多数是血管紧张素I转化酶(ACE)抑制剂和血管紧张素受体I型(AT1R)拮抗剂。但是,血管紧张素肽也可以结合不同于AT1R的受体,特别是II型血管紧张素受体(AT2R),从而导致其与AT1R结合的生物学和生理作用不同,有时甚至是拮抗作用。在本《观点》中,将对RAS的组成部分以及为控制它而开发的治疗工具进行审查。特别是,将讨论AT2R的特性和调节其功能的工具。AT2R激动剂或拮抗剂是心血管疾病的潜在治疗剂,用于激动剂和用于控制疼痛的拮抗剂。然而,必须优化控制它们的结合特性和将它们靶向靶组织。
更新日期:2020-02-21
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