INSERM U955, 94700, Creteil, France.
Universite Paris-Est Creteil Val-de-Marne, 94700, Creteil, France.
Curr Pharm Des. 2017;23(40):6215-6222. doi: 10.2174/1381612823666170622112253.
NO produced by eNOS plays important roles in the cardiovascular system. Alterations in eNOS activity and expression occur in various cardiovascular disorders and eNOS constitutes a therapeutic target. In addition to posttranslational modifications of eNOS that affect eNOS activity, transcriptional and post-transcriptional regulation of eNOS expression also controls eNOS-derived NO production. Bradykinin is an important determinant of vascular function and participates in the regulation of eNOS activity and expression. A number of currently used drugs or investigational molecules targeting specific ion channels, enzymes or receptors, including dihydropyridine calcium channel blockers, angiotensin-converting enzyme inhibitors, statins, AT1 receptor blockers and angiotensin-(1-7), increase eNOS expression and activity. In this context, activation of bradykinin B2 receptors appears to be a common step for these drugs to promote eNOS expression, which certainly contributes to their therapeutic actions.
内皮型一氧化氮合酶（eNOS）产生的一氧化氮在心血管系统中发挥着重要作用。eNOS 活性和表达的改变发生在各种心血管疾病中，eNOS 构成了治疗靶点。除了影响 eNOS 活性的 eNOS 的翻译后修饰外，eNOS 表达的转录和转录后调节也控制 eNOS 衍生的 NO 产生。缓激肽是血管功能的重要决定因素，并参与 eNOS 活性和表达的调节。目前使用的许多药物或针对特定离子通道、酶或受体的研究分子，包括二氢吡啶钙通道阻滞剂、血管紧张素转换酶抑制剂、他汀类药物、AT1 受体阻滞剂和血管紧张素-(1-7)，增加 eNOS 的表达和活性。在这种情况下，缓激肽 B2 受体的激活似乎是这些药物促进 eNOS 表达的共同步骤，这肯定有助于它们的治疗作用。
