Sisson T H, Simon R H
Division of Pulmonary and Critical Care Medicine, Department of Internal Medicine, University of Michigan Health Sciences Center, Ann Arbor, MI 48109-0642, USA.
Curr Drug Targets. 2007 Sep;8(9):1016-29. doi: 10.2174/138945007781662319.
The importance of the plasminogen activator (PA) system in multiple pulmonary disorders has become increasingly apparent as methods to analyze its components have improved. Early investigations discovered that the pulmonary alveolar space is normally a pro-fibrinolytic environment that is diminished in a variety of lung diseases. Interest in these observations was greatly increased when animal experiments revealed that manipulations of the PA system significantly modulated the tissue fibrosis that follows many types of lung injury. In particular, enhancement of PA activity was found to consistently decrease the extent of scarring induced by lung damage. Based upon these early observations, it was hypothesized that fibrin was necessary for the pathogenesis of lung fibrosis, and that an increase in PA activity would reduce collagen accumulation by accelerating the clearance of fibrin from the provisional matrix. However, as is often the case with simple hypotheses, subsequent studies revealed that the actual role of the PA system in pulmonary disease is much more complex. Possible mechanisms beyond fibrinolysis include degradation of other matrix proteins, activation of protease cascades including those involving matrix metalloproteinases, activation and release of growth factors from sites of production and sequestration, and modulation of cell adhesion and motility. In each of these processes, the serpin plasminogen activator inhibitor-1 (PAI-1) plays a central role. For these reasons, it has become apparent that PAI-1 presents an attractive target to influence multiple disease processes within the lung, particularly those that lead to lung fibrosis.
随着分析纤溶酶原激活剂(PA)系统各成分的方法不断改进,该系统在多种肺部疾病中的重要性日益凸显。早期研究发现,肺泡腔通常是一个促纤溶环境,而在多种肺部疾病中这一环境会减弱。当动物实验表明对PA系统的操作能显著调节多种类型肺损伤后的组织纤维化时,人们对这些观察结果的兴趣大增。特别是,发现增强PA活性可持续降低肺损伤所致的瘢痕形成程度。基于这些早期观察结果,有人提出假设,即纤维蛋白是肺纤维化发病机制所必需的,而PA活性增加会通过加速从临时基质中清除纤维蛋白来减少胶原蛋白的积累。然而,正如简单假设常出现的情况一样,后续研究表明PA系统在肺部疾病中的实际作用要复杂得多。除纤维蛋白溶解外的可能机制包括其他基质蛋白的降解、蛋白酶级联反应(包括涉及基质金属蛋白酶的反应)的激活、生长因子从产生和储存部位的激活与释放,以及细胞黏附和运动的调节。在这些过程中,丝氨酸蛋白酶抑制剂纤溶酶原激活剂抑制剂-1(PAI-1)都起着核心作用。基于这些原因,很明显PAI-1是影响肺部多种疾病进程,尤其是那些导致肺纤维化的疾病进程的一个有吸引力的靶点。