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Human-based evidence for the therapeutic potential of arginase inhibitors in cardiovascular diseases
Drug Discovery Today ( IF 6.5 ) Pub Date : 2020-11-13 , DOI: 10.1016/j.drudis.2020.11.005
Johnny Moretto 1 , Marc Pudlo 1 , Céline Demougeot 1
Affiliation  

Arginase is a ubiquitous enzyme that regulates polyamine- and nitric-oxide-requiring vascular functions. It is well-established that, in mammals, arginase overactivation contributes to endothelial dysfunction, a hallmark of cardiovascular diseases. The pharmacological potential of arginase inhibition for improving vascular function is largely supported by a wide range of data from animal studies. However, caution is required before extrapolating animal data to humans because interspecies differences in arginase expression and localization have been observed. For this reason, this review presents the existing arguments from human data in favor of a role of arginase in cardiovascular diseases. Then, the available data from clinical studies are discussed, as well as the possible arginase inhibitors that might be used in future large-scale clinical trials.



中文翻译:

精氨酸酶抑制剂在心血管疾病中的治疗潜力的人类证据

精氨酸酶是一种普遍存在的酶,可调节需要多胺和一氧化氮的血管功能。众所周知,在哺乳动物中,精氨酸酶过度激活会导致内皮功能障碍,这是心血管疾病的标志。来自动物研究的广泛数据在很大程度上支持精氨酸酶抑制改善血管功能的药理学潜力。然而,在将动物数据外推到人类之前需要谨慎,因为已经观察到精氨酸酶表达和定位的种间差异。出于这个原因,本综述提出了来自人类数据的现有论据,支持精氨酸酶在心血管疾病中的作用。然后,讨论来自临床研究的可用数据,

更新日期:2020-11-13
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