Berk B C
University of Rochester, Department of Medicine, New York 14642, USA.
J Am Soc Nephrol. 1999 Jan;10 Suppl 11:S62-8.
In this review, the signal events regulated by angiotensin II (AngII) in vascular smooth muscle are analyzed based on activation of specific tyrosine kinases. AngII has been shown to play a critical role in the pathogenesis of hypertension, inflammation, atherosclerosis, and congestive heart failure. The expanding role of AngII indicates that multiple signal transduction pathways are likely to be activated in a tissue-specific manner. Although at least three AngII receptors have been characterized, it seems that the AngII type I receptor (AT1R) is physiologically most important since pharmacologic inhibitors of the AT1R block most AngII signal events and have beneficial effects on cardiovascular disease. The AT1R is a seven transmembrane-spanning G protein-coupled receptor that regulates intracellular signal events by activation of Gq and Gi. However, many recent data indicate that activation of tyrosine kinases by several different mechanisms contributes to AngII effects in target tissues. Tyrosine kinases activated by AngII include c-Src, focal adhesion kinase (FAK), Pyk2 (CADTK), Janus kinases (JAK2 and TYK2), and the receptor tyrosine kinases Ax1, epidermal growth factor, and platelet-derived growth factor. Finally, unknown tyrosine kinases may mediate tyrosine phosphorylation of paxillin, Shc, Raf, and phospholipase C-gamma after AngII stimulation. These AngII-regulated tyrosine kinases seem to be required for AngII effects such as vasoconstriction, proto-oncogene expression, and protein synthesis based on studies with tyrosine kinase inhibitors. Thus, understanding AngII-stimulated signaling events, especially those related to tyrosine kinase activity, may form the basis for the development of new therapies for cardiovascular diseases.
在本综述中,基于特定酪氨酸激酶的激活情况,对血管平滑肌中由血管紧张素II(AngII)调节的信号事件进行了分析。已证明AngII在高血压、炎症、动脉粥样硬化和充血性心力衰竭的发病机制中起关键作用。AngII作用的不断扩展表明,多种信号转导途径可能以组织特异性方式被激活。尽管至少已鉴定出三种AngII受体,但似乎AngII 1型受体(AT1R)在生理上最为重要,因为AT1R的药理抑制剂可阻断大多数AngII信号事件,并对心血管疾病具有有益作用。AT1R是一种七跨膜G蛋白偶联受体,通过激活Gq和Gi来调节细胞内信号事件。然而,最近的许多数据表明,几种不同机制激活酪氨酸激酶有助于AngII在靶组织中的作用。由AngII激活的酪氨酸激酶包括c-Src、粘着斑激酶(FAK)、Pyk2(CADTK)、Janus激酶(JAK2和TYK2),以及受体酪氨酸激酶Ax1、表皮生长因子和血小板衍生生长因子。最后,未知的酪氨酸激酶可能在AngII刺激后介导桩蛋白、Shc、Raf和磷脂酶C-γ的酪氨酸磷酸化。基于酪氨酸激酶抑制剂的研究,这些受AngII调节的酪氨酸激酶似乎是AngII产生诸如血管收缩、原癌基因表达和蛋白质合成等作用所必需的。因此,了解AngII刺激的信号事件,尤其是那些与酪氨酸激酶活性相关的事件,可能为开发心血管疾病的新疗法奠定基础。